ChEMBL ligand: CHEMBL3301607 (Filgotinib, G-146034, G146034, Glpg-0634, GLPG0634, GS-6034 FREE BASE)
26S proteasome regulatory subunit 6B in Human [ChEMBL: CHEMBL3831205] [UniProtKB: P43686] There should be some charts here, you may need to enable JavaScript!
protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] There should be some charts here, you may need to enable JavaScript!
protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619] There should be some charts here, you may need to enable JavaScript!
protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0] There should be some charts here, you may need to enable JavaScript!
aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2] There should be some charts here, you may need to enable JavaScript!
Actin-related protein 2 in Human [ChEMBL: CHEMBL6090] [UniProtKB: P61160] There should be some charts here, you may need to enable JavaScript!
Actin-related protein 3 in Human [ChEMBL: CHEMBL4105857] [UniProtKB: P61158] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] There should be some charts here, you may need to enable JavaScript!
activin A receptor type 1/Activin receptor type-1 in Human [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] There should be some charts here, you may need to enable JavaScript!
activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] There should be some charts here, you may need to enable JavaScript!
activin A receptor type 2B/Activin receptor type-2B in Human [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705] There should be some charts here, you may need to enable JavaScript!
Acyl-CoA dehydrogenase family member 10 in Human [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1] There should be some charts here, you may need to enable JavaScript!
Acyl-CoA dehydrogenase family member 11 in Human [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0] There should be some charts here, you may need to enable JavaScript!
Adenine phosphoribosyltransferase in Human [ChEMBL: CHEMBL4105819] [UniProtKB: P07741] There should be some charts here, you may need to enable JavaScript!
Adenosine kinase in Human [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263] There should be some charts here, you may need to enable JavaScript!
Adenylate kinase 2, mitochondrial in Human [ChEMBL: CHEMBL4938] [UniProtKB: P54819] There should be some charts here, you may need to enable JavaScript!
Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141] There should be some charts here, you may need to enable JavaScript!
Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236] There should be some charts here, you may need to enable JavaScript!
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
AP2 associated kinase 1/AP2-associated protein kinase 1 in Human [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8] There should be some charts here, you may need to enable JavaScript!
ATP-dependent 6-phosphofructokinase, platelet type in Human [ChEMBL: CHEMBL2972] [UniProtKB: Q01813] There should be some charts here, you may need to enable JavaScript!
ATP-dependent RNA helicase DDX1 in Human [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499] There should be some charts here, you may need to enable JavaScript!
ATP-dependent RNA helicase DDX3X in Human [ChEMBL: CHEMBL5553] [UniProtKB: O00571] There should be some charts here, you may need to enable JavaScript!
ATP-dependent RNA helicase DDX42 in Human [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3] There should be some charts here, you may need to enable JavaScript!
ATP-dependent RNA helicase DHX30 in Human [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3] There should be some charts here, you may need to enable JavaScript!
coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60] There should be some charts here, you may need to enable JavaScript!
aurora kinase A/Aurora kinase A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] There should be some charts here, you may need to enable JavaScript!
aurora kinase B/Aurora kinase B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] There should be some charts here, you may need to enable JavaScript!
beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] There should be some charts here, you may need to enable JavaScript!
Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human [ChEMBL: CHEMBL5922] [UniProtKB: P22234] There should be some charts here, you may need to enable JavaScript!
BMP2 inducible kinase/BMP-2-inducible protein kinase in Human [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1] There should be some charts here, you may need to enable JavaScript!
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] There should be some charts here, you may need to enable JavaScript!
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] There should be some charts here, you may need to enable JavaScript!
bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873] There should be some charts here, you may need to enable JavaScript!
BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] There should be some charts here, you may need to enable JavaScript!
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] There should be some charts here, you may need to enable JavaScript!
protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694] There should be some charts here, you may need to enable JavaScript!
protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612] There should be some charts here, you may need to enable JavaScript!
protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 delta/Casein kinase I isoform delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] There should be some charts here, you may need to enable JavaScript!
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] There should be some charts here, you may need to enable JavaScript!
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] There should be some charts here, you may need to enable JavaScript!
Choline-phosphate cytidylyltransferase A in Human [ChEMBL: CHEMBL4105855] [UniProtKB: P49585] There should be some charts here, you may need to enable JavaScript!
Chromodomain-helicase-DNA-binding protein 4 in Human [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839] There should be some charts here, you may need to enable JavaScript!
citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] There should be some charts here, you may need to enable JavaScript!
cyclin G associated kinase/Cyclin-G-associated kinase in Human [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976] There should be some charts here, you may need to enable JavaScript!
Cytochrome c1, heme protein, mitochondrial in Human [ChEMBL: CHEMBL4105975] [UniProtKB: P08574] There should be some charts here, you may need to enable JavaScript!
dCTP pyrophosphatase 1 in Human [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773] There should be some charts here, you may need to enable JavaScript!
death associated protein kinase 1/Death-associated protein kinase 1 in Human [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355] There should be some charts here, you may need to enable JavaScript!
Delta(24)-sterol reductase in Human [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392] There should be some charts here, you may need to enable JavaScript!
Deoxycytidine kinase in Human [ChEMBL: CHEMBL2447] [UniProtKB: P27707] There should be some charts here, you may need to enable JavaScript!
discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] There should be some charts here, you may need to enable JavaScript!
DnaJ homolog subfamily A member 1 in Human [ChEMBL: CHEMBL2189122] [UniProtKB: P31689] There should be some charts here, you may need to enable JavaScript!
DNA replication licensing factor MCM4 in Human [ChEMBL: CHEMBL4105745] [UniProtKB: P33991] There should be some charts here, you may need to enable JavaScript!
DNA topoisomerase 2-beta in Human [ChEMBL: CHEMBL3396] [UniProtKB: Q02880] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] There should be some charts here, you may need to enable JavaScript!
testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] There should be some charts here, you may need to enable JavaScript!
Dynamin-like GTPase OPA1, mitochondrial in Human [ChEMBL: CHEMBL4105705] [UniProtKB: O60313] There should be some charts here, you may need to enable JavaScript!
TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] There should be some charts here, you may need to enable JavaScript!
Electron transfer flavoprotein subunit beta in Human [ChEMBL: CHEMBL4105744] [UniProtKB: P38117] There should be some charts here, you may need to enable JavaScript!
Elongation factor Tu, mitochondrial in Human [ChEMBL: CHEMBL4105970] [UniProtKB: P49411] There should be some charts here, you may need to enable JavaScript!
EPH receptor A1/Ephrin type-A receptor 1 in Human [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] There should be some charts here, you may need to enable JavaScript!
EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] There should be some charts here, you may need to enable JavaScript!
EPH receptor A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] There should be some charts here, you may need to enable JavaScript!
EPH receptor A5/Ephrin type-A receptor 5 in Human [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] There should be some charts here, you may need to enable JavaScript!
EPH receptor A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] There should be some charts here, you may need to enable JavaScript!
EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] There should be some charts here, you may need to enable JavaScript!
EPH receptor B3/Ephrin type-B receptor 3 in Human [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] There should be some charts here, you may need to enable JavaScript!
EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] There should be some charts here, you may need to enable JavaScript!
EPH receptor B6/Ephrin type-B receptor 6 in Human [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] There should be some charts here, you may need to enable JavaScript!
eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3] There should be some charts here, you may need to enable JavaScript!
Eukaryotic translation initiation factor 5B in Human [ChEMBL: CHEMBL4105852] [UniProtKB: O60841] There should be some charts here, you may need to enable JavaScript!
Exosome RNA helicase MTR4 in Human [ChEMBL: CHEMBL4105889] [UniProtKB: P42285] There should be some charts here, you may need to enable JavaScript!
Ferrochelatase, mitochondrial in Human [ChEMBL: CHEMBL3879831] [UniProtKB: P22830] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] There should be some charts here, you may need to enable JavaScript!
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] There should be some charts here, you may need to enable JavaScript!
General transcription and DNA repair factor IIH helicase subunit XPD in Human [ChEMBL: CHEMBL4105743] [UniProtKB: P18074] There should be some charts here, you may need to enable JavaScript!
Glycine--tRNA ligase in Human [ChEMBL: CHEMBL4105815] [UniProtKB: P41250] There should be some charts here, you may need to enable JavaScript!
Glycogen phosphorylase, brain form in Human [ChEMBL: CHEMBL3856] [UniProtKB: P11216] There should be some charts here, you may need to enable JavaScript!
Glycogen phosphorylase, liver form in Human [ChEMBL: CHEMBL2568] [UniProtKB: P06737] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] There should be some charts here, you may need to enable JavaScript!
GTP-binding nuclear protein Ran in Human [ChEMBL: CHEMBL1741190] [UniProtKB: P62826] There should be some charts here, you may need to enable JavaScript!
GTP-binding protein 4 in Human [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4] There should be some charts here, you may need to enable JavaScript!
Haem oxygenase 2/Heme oxygenase 2 in Human [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519] There should be some charts here, you may need to enable JavaScript!
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6] There should be some charts here, you may need to enable JavaScript!
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] There should be some charts here, you may need to enable JavaScript!
inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268] There should be some charts here, you may need to enable JavaScript!
Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] There should be some charts here, you may need to enable JavaScript!
Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] There should be some charts here, you may need to enable JavaScript!
integrin linked kinase/Integrin-linked protein kinase in Human [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418] There should be some charts here, you may need to enable JavaScript!
interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] There should be some charts here, you may need to enable JavaScript!
interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616] There should be some charts here, you may need to enable JavaScript!
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3] There should be some charts here, you may need to enable JavaScript!
Isoleucine--tRNA ligase, mitochondrial in Human [ChEMBL: CHEMBL4105821] [UniProtKB: Q9NSE4] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597] There should be some charts here, you may need to enable JavaScript!
Jak1 protein in Rat [ChEMBL: CHEMBL3351191] [UniProtKB: Q5FVF5] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human [ChEMBL: CHEMBL3038492] [GtoPdb: 2048, 2047] [UniProtKB: O60674, P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333] There should be some charts here, you may need to enable JavaScript!
LIM domain kinase 1 in Human [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] There should be some charts here, you may need to enable JavaScript!
LIM domain kinase 2 in Human [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] There should be some charts here, you may need to enable JavaScript!
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] There should be some charts here, you may need to enable JavaScript!
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] There should be some charts here, you may need to enable JavaScript!
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] There should be some charts here, you may need to enable JavaScript!
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] There should be some charts here, you may need to enable JavaScript!
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] There should be some charts here, you may need to enable JavaScript!
microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] There should be some charts here, you may need to enable JavaScript!
microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] There should be some charts here, you may need to enable JavaScript!
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] There should be some charts here, you may need to enable JavaScript!
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] There should be some charts here, you may need to enable JavaScript!
Membrane-associated progesterone receptor component 1 in Human [ChEMBL: CHEMBL4105706] [UniProtKB: O00264] There should be some charts here, you may need to enable JavaScript!
protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] There should be some charts here, you may need to enable JavaScript!
Midasin in Human [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22] There should be some charts here, you may need to enable JavaScript!
misshapen like kinase 1/Misshapen-like kinase 1 in Human [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5] There should be some charts here, you may need to enable JavaScript!
ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4] There should be some charts here, you may need to enable JavaScript!
BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] There should be some charts here, you may need to enable JavaScript!
Myosin-10 in Human [ChEMBL: CHEMBL4105746] [UniProtKB: P35580] There should be some charts here, you may need to enable JavaScript!
Myosin-14 in Human [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406] There should be some charts here, you may need to enable JavaScript!
myosin light chain kinase 3/Myosin light chain kinase in Human [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0] There should be some charts here, you may need to enable JavaScript!
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] There should be some charts here, you may need to enable JavaScript!
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] There should be some charts here, you may need to enable JavaScript!
NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] There should be some charts here, you may need to enable JavaScript!
Obg-like ATPase 1 in Human [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5] There should be some charts here, you may need to enable JavaScript!
Peroxisomal acyl-coenzyme A oxidase 1 in Human [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067] There should be some charts here, you may need to enable JavaScript!
Peroxisomal acyl-coenzyme A oxidase 3 in Human [ChEMBL: CHEMBL4105817] [UniProtKB: O15254] There should be some charts here, you may need to enable JavaScript!
Phenylalanine--tRNA ligase beta subunit in Human [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9] There should be some charts here, you may need to enable JavaScript!
Phosphatidylethanolamine-binding protein 1 in Human [ChEMBL: CHEMBL4105856] [UniProtKB: P30086] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-5-phosphate 4-kinase type 2 alpha/Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha in Human [ChEMBL: CHEMBL1795194] [GtoPdb: 2858] [UniProtKB: P48426] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8] There should be some charts here, you may need to enable JavaScript!
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] There should be some charts here, you may need to enable JavaScript!
Probable ATP-dependent RNA helicase DDX6 in Human [ChEMBL: CHEMBL4105783] [UniProtKB: P26196] There should be some charts here, you may need to enable JavaScript!
protein kinase C alpha/Protein kinase C alpha type in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] There should be some charts here, you may need to enable JavaScript!
protein kinase C beta/Protein kinase C beta type in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] There should be some charts here, you may need to enable JavaScript!
protein kinase C delta/Protein kinase C delta type in Human [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] There should be some charts here, you may need to enable JavaScript!
protein kinase C iota/Protein kinase C iota type in Human [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] There should be some charts here, you may need to enable JavaScript!
protein kinase C theta/Protein kinase C theta type in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] There should be some charts here, you may need to enable JavaScript!
protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] There should be some charts here, you may need to enable JavaScript!
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] There should be some charts here, you may need to enable JavaScript!
Putative heat shock protein HSP 90-beta 2 in Human [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8] There should be some charts here, you may need to enable JavaScript!
Pyridoxal kinase in Human [ChEMBL: CHEMBL1075181] [UniProtKB: O00764] There should be some charts here, you may need to enable JavaScript!
Rab-like protein 3 in Human [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] There should be some charts here, you may need to enable JavaScript!
Ras-related C3 botulinum toxin substrate 1 in Human [ChEMBL: CHEMBL6094] [UniProtKB: P63000] There should be some charts here, you may need to enable JavaScript!
Ras-related protein Rab-10 in Human [ChEMBL: CHEMBL4105971] [UniProtKB: P61026] There should be some charts here, you may need to enable JavaScript!
RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159] There should be some charts here, you may need to enable JavaScript!
Ras-related protein Rab-6A in Human [ChEMBL: CHEMBL4105703] [UniProtKB: P20340] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] There should be some charts here, you may need to enable JavaScript!
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] There should be some charts here, you may need to enable JavaScript!
Ribosyldihydronicotinamide dehydrogenase [quinone] in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083] There should be some charts here, you may need to enable JavaScript!
RNA cytidine acetyltransferase in Human [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0] There should be some charts here, you may need to enable JavaScript!
S-adenosylmethionine synthase isoform type-2 in Human [ChEMBL: CHEMBL3313835] [UniProtKB: P31153] There should be some charts here, you may need to enable JavaScript!
Septin-9 in Human [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] There should be some charts here, you may need to enable JavaScript!
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] There should be some charts here, you may need to enable JavaScript!
Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] There should be some charts here, you may need to enable JavaScript!
A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] There should be some charts here, you may need to enable JavaScript!
ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] There should be some charts here, you may need to enable JavaScript!
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] There should be some charts here, you may need to enable JavaScript!
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] There should be some charts here, you may need to enable JavaScript!
protein kinase D2/Serine/threonine-protein kinase D2 in Human [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] There should be some charts here, you may need to enable JavaScript!
protein kinase D3/Serine/threonine-protein kinase D3 in Human [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] There should be some charts here, you may need to enable JavaScript!
endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460] There should be some charts here, you may need to enable JavaScript!
endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5] There should be some charts here, you may need to enable JavaScript!
ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9] There should be some charts here, you may need to enable JavaScript!
large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] There should be some charts here, you may need to enable JavaScript!
microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] There should be some charts here, you may need to enable JavaScript!
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] There should be some charts here, you may need to enable JavaScript!
CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] There should be some charts here, you may need to enable JavaScript!
CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] There should be some charts here, you may need to enable JavaScript!
protein kinase N1/Serine/threonine-protein kinase N1 in Human [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] There should be some charts here, you may need to enable JavaScript!
protein kinase N2/Serine/threonine-protein kinase N2 in Human [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] There should be some charts here, you may need to enable JavaScript!
nemo like kinase/Serine/threonine-protein kinase NLK in Human [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] There should be some charts here, you may need to enable JavaScript!
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] There should be some charts here, you may need to enable JavaScript!
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] There should be some charts here, you may need to enable JavaScript!
p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5] There should be some charts here, you may need to enable JavaScript!
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] There should be some charts here, you may need to enable JavaScript!
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] There should be some charts here, you may need to enable JavaScript!
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] There should be some charts here, you may need to enable JavaScript!
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] There should be some charts here, you may need to enable JavaScript!
salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] There should be some charts here, you may need to enable JavaScript!
SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2] There should be some charts here, you may need to enable JavaScript!
serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] There should be some charts here, you may need to enable JavaScript!
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] There should be some charts here, you may need to enable JavaScript!
TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54] There should be some charts here, you may need to enable JavaScript!
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] There should be some charts here, you may need to enable JavaScript!
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2] There should be some charts here, you may need to enable JavaScript!
unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] There should be some charts here, you may need to enable JavaScript!
unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2] There should be some charts here, you may need to enable JavaScript!
Signal recognition particle receptor subunit alpha in Human [ChEMBL: CHEMBL4105934] [UniProtKB: P08240] There should be some charts here, you may need to enable JavaScript!
STE20 like kinase/STE20-like serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] There should be some charts here, you may need to enable JavaScript!
STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6] There should be some charts here, you may need to enable JavaScript!
Structural maintenance of chromosomes protein 1A in Human [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683] There should be some charts here, you may need to enable JavaScript!
Structural maintenance of chromosomes protein 2 in Human [ChEMBL: CHEMBL4105890] [UniProtKB: O95347] There should be some charts here, you may need to enable JavaScript!
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] There should be some charts here, you may need to enable JavaScript!
TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] There should be some charts here, you may need to enable JavaScript!
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] There should be some charts here, you may need to enable JavaScript!
ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] There should be some charts here, you may need to enable JavaScript!
FER tyrosine kinase/Tyrosine-protein kinase Fer in Human [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] There should be some charts here, you may need to enable JavaScript!
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] There should be some charts here, you may need to enable JavaScript!
fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] There should be some charts here, you may need to enable JavaScript!
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] There should be some charts here, you may need to enable JavaScript!
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] There should be some charts here, you may need to enable JavaScript!
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] There should be some charts here, you may need to enable JavaScript!
MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] There should be some charts here, you may need to enable JavaScript!
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] There should be some charts here, you may need to enable JavaScript!
tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] There should be some charts here, you may need to enable JavaScript!
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] There should be some charts here, you may need to enable JavaScript!
Tyrosine--tRNA ligase, cytoplasmic in Human [ChEMBL: CHEMBL3179] [UniProtKB: P54577] There should be some charts here, you may need to enable JavaScript!
U5 small nuclear ribonucleoprotein 200 kDa helicase in Human [ChEMBL: CHEMBL4105972] [UniProtKB: O75643] There should be some charts here, you may need to enable JavaScript!
UMP-CMP kinase in Human [ChEMBL: CHEMBL5681] [UniProtKB: P30085] There should be some charts here, you may need to enable JavaScript!
aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3] There should be some charts here, you may need to enable JavaScript!
Uncharacterized protein FLJ45252 in Human [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] There should be some charts here, you may need to enable JavaScript!
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human [ChEMBL: CHEMBL4105892] [UniProtKB: P49748] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
26S proteasome regulatory subunit 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831205] [UniProtKB: P43686]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.69	pKd	2028	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Acyl-CoA dehydrogenase family member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Acyl-CoA dehydrogenase family member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Adenylate kinase 2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.3	pKd	4990	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATP-dependent 6-phosphofructokinase, platelet type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2972] [UniProtKB: Q01813]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of AURORA-B (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.18	pKd	6590	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.44	pKd	3633	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of CSNK1G2 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Choline-phosphate cytidylyltransferase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105855] [UniProtKB: P49585]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of CDK2 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
dCTP pyrophosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
death associated protein kinase 1/Death-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2558] [GtoPdb: 2002] [UniProtKB: P53355]
ChEMBL	Inhibition of DAPK1 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Delta(24)-sterol reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
DnaJ homolog subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189122] [UniProtKB: P31689]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
DNA replication licensing factor MCM4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105745] [UniProtKB: P33991]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
DNA topoisomerase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Dynamin-like GTPase OPA1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105705] [UniProtKB: O60313]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Electron transfer flavoprotein subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105744] [UniProtKB: P38117]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of EPHA5 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Eukaryotic translation initiation factor 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105852] [UniProtKB: O60841]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Exosome RNA helicase MTR4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105889] [UniProtKB: P42285]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Ferrochelatase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879831] [UniProtKB: P22830]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
General transcription and DNA repair factor IIH helicase subunit XPD in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105743] [UniProtKB: P18074]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Glycine--tRNA ligase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105815] [UniProtKB: P41250]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Glycogen phosphorylase, brain form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3856] [UniProtKB: P11216]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Glycogen phosphorylase, liver form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
GTP-binding nuclear protein Ran in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741190] [UniProtKB: P62826]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
GTP-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Haem oxygenase 2/Heme oxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
homeodomain interacting protein kinase 2/Homeodomain-interacting protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4576] [GtoPdb: 2034] [UniProtKB: Q9H2X6]
ChEMBL	Inhibition of HIPK2 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.33	pKd	4714	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of IRAK4 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Isoleucine--tRNA ligase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105821] [UniProtKB: Q9NSE4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597]
GtoPdb	-	-	5.59	pIC50	2600	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb	-	-	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1/JAK2/TYK2 in human whole blood assessed as inhibition of IL-6-induced STAT-1 phosphorylation preincubated for 45 mins followed by IL-6 addition measured after 15 mins by FACS analysis	B	6.04	pIC50	918	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of JAK1/JAK2/TYK2 signalling in human whole blood assessed as inhibition of IL-6 stimulated STAT1 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IL-6 stimulation and incubated for 20 mins by flow cytometry analysis	B	6.39	pIC50	407.4	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
GtoPdb	-	-	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb	-	-	6.94	pIC50	116	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
GtoPdb	-	-	7.49	pIC50	28	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
GtoPdb	-	-	7.96	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
Jak1 protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351191] [UniProtKB: Q5FVF5]
ChEMBL	Inhibition of rat JAK1	B	7.54	pIC50	29	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597]
GtoPdb	-	-	5.59	pIC50	2600	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as inhibition of IFN-alpha-induced STAT-3 phosphorylation preincubated for 45 mins followed by IFN-alpha addition measured after 15 mins by FACS analysis	B	5.82	pIC50	1500	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis	B	5.95	pIC50	1127.2	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT1 phosphorylation preincubated for 30 mins followed by IFNalpha addition and measured after 20 mins by flow cytometer analysis	B	5.95	pIC50	1127	nM	IC50	J Med Chem (2024) 67: 8545-8568 [PMID:38805213]
ChEMBL	Inhibition of JAK1/TYK2 signaling pathway in human U2OS cells assessed as reduction in IFN-alphaB2-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by IFN-alphaB2 addition and measured after 1 hr by TR-FRET analysis	B	6.33	pIC50	467.74	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/TYK2 signaling pathway in human U2OS cells assessed as reduction in IFN-alphaB2-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by IFN-alphaB2 addition and measured after 1 hr by TR-FRET analysis	B	6.36	pIC50	436	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1	B	6.36	pIC50	436	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb	-	-	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1/TYK2 signalling in human whole blood assessed as inhibition of IFN-alpha stimulated STAT1 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IFN-alpha stimulation and incubated for 20 mins by flow cytometry analysis	B	6.51	pIC50	306.2	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
GtoPdb	-	-	6.94	pIC50	116	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
GtoPdb	-	-	7.96	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis	B	8.95	pIC50	1.13	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038492] [GtoPdb: 2048, 2047] [UniProtKB: O60674, P23458]
ChEMBL	Inhibition of JAK1/JAK2 signaling pathway in human U2OS cells assessed as reduction in IFN-gamma-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by IFN-gamma addition and measured after 1 hr by TR-FRET analysis	B	5.47	pIC50	3388.44	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1	B	5.47	pIC50	3364	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK1/JAK2 signaling pathway in human U2OS cells assessed as reduction in IFN-gamma-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by IFN-gamma addition and measured after 1 hr by TR-FRET analysis	B	5.47	pIC50	3364	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
GtoPdb	-	-	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter	B	5.98	pIC50	1045	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK1/JAK2 signaling pathway in human HeLa cells assessed as reduction in OSM-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by OSM addition and measured after 20 mins by luciferase based analysis	B	5.98	pIC50	1045	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK2 signaling pathway in human HeLa cells assessed as reduction in OSM-induced STAT1 phosphorylation preincubated with compound for 1 hr followed by OSM addition and measured after 20 mins by luciferase based analysis	B	6.01	pIC50	977.24	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
GtoPdb	-	-	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb	-	-	7.49	pIC50	28	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
GtoPdb	-	-	7.96	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597]
ChEMBL	Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-12-induced STAT-4 phosphorylation preincubated for 45 mins followed by IL-12 addition measured after 15 mins by FACS analysis	B	4.87	pIC50	13362	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of JAK2/TYK2 in human whole blood assessed as inhibition of IL-23-induced STAT-3 phosphorylation preincubated for 45 mins followed by IL-23 addition measured after 15 mins by FACS analysis	B	4.99	pIC50	10123	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb	-	-	5.59	pIC50	2600	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb	-	-	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
GtoPdb	-	-	6.94	pIC50	116	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
GtoPdb	-	-	7.49	pIC50	28	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333]
ChEMBL	Inhibition of JAK1/JAK3 in human whole blood assessed as inhibition of IL-15-induced STAT-5 phosphorylation preincubated for 45 mins followed by IL-15 addition measured after 15 mins by FACS analysis	B	5.67	pIC50	2140	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis	B	5.75	pIC50	1790.61	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis	B	5.75	pIC50	1789	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2 induced STAT5 phosphorylation preincubated for 30 mins followed by IIL-2 addition and measured after 20 mins by flow cytometer analysis	B	5.95	pIC50	1127	nM	IC50	J Med Chem (2024) 67: 8545-8568 [PMID:38805213]
ChEMBL	Inhibition of JAK1/JAK3 signalling in human whole blood assessed as inhibition of IL-2 stimulated STAT5 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IL-2 stimulation and incubated for 20 mins by flow cytometry analysis	B	6.09	pIC50	820.4	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
GtoPdb	-	-	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1/JAK3 signaling pathway in human NK92 cells assessed as reduction in IL-2 induced STAT5 phosphorylation preincubated with compound for 1 hr followed by IL-2 addition and measured after 20 mins by Alphascreen analysis	B	6.46	pIC50	346.74	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
GtoPdb	-	-	6.52	pIC50	810	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6	B	6.81	pIC50	154	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK1/JAK3 signaling pathway in human NK92 cells assessed as reduction in IL-2 induced STAT5 phosphorylation preincubated with compound for 1 hr followed by IL-2 addition and measured after 20 mins by Alphascreen analysis	B	6.83	pIC50	148	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1/JAK3 in IL2-induced human NK92 cells assessed as pSTAT5	B	6.83	pIC50	148	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
GtoPdb	-	-	7.96	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL	Inhibition of human CSF1R (unknown origin)	B	6.31	pIC50	489	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Selectivity interaction (Radioactive biochemical assays (Millipore and Galapagos N.V.)) EUB0000626a CSF1R	B	6.31	pIC50	488.9	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of FMS (unknown origin)	B	6.31	pIC50	488.9	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL	Inhibition of MNK2 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL	Inhibition of cKIT (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Membrane-associated progesterone receptor component 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105706] [UniProtKB: O00264]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Midasin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of MINK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.67	pKd	2140	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 12/Mitogen-activated protein kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4674] [GtoPdb: 1501] [UniProtKB: P53778]
ChEMBL	Inhibition of MAPK12 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of MAPK14 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of MAP3K3 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318]
ChEMBL	Inhibition of TAK1 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of GCK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of MAP4K4 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Myosin-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105746] [UniProtKB: P35580]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
myosin light chain kinase 3/Myosin light chain kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of recombinant human Tyk2 expressed in sf21 baculovirus expression system assessed as phosphorylation level in presence of 1 mM ATP	B	5.59	pIC50	2600	nM	IC50	Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659]
ChEMBL	Inhibition of TYK2 (unknown origin)	B	5.59	pIC50	2600	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb	-	-	5.59	pIC50	2600	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	6.11	pIC50	780	nM	IC50	US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s).	B	6.11	pIC50	780	nM	IC50	US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	6.11	pIC50	780	nM	IC50	US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL	Inhibition of Tyk2 (unknown origin)	B	6.94	pIC50	116	nM	IC50	J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL	Inhibition of human TYK2 using GGMEDIYFEFMGGKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method	B	6.94	pIC50	116	nM	IC50	Medchemcomm (2018) 9: 477-489 [PMID:30108938]
ChEMBL	Selectivity interaction (Radiometric kinase assay) EUB0000626a TYK2	B	6.94	pIC50	116	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of recombinant TYK2 (unknown origin) in the presence of ATP	B	6.94	pIC50	116	nM	IC50	Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL	Inhibition of recombinant human TYK2 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate preincubated with compound for 60 mins followed by substrate addition and measured after 90 mins in presence of ATP	B	6.94	pIC50	116	nM	IC50	Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL	Inhibition of TYK2 (unknown origin)	B	6.94	pIC50	116	nM	IC50	Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL	Inhibition of human recombinant TYK2 incubated for 60 mins	B	6.94	pIC50	116	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Selectivity interaction (Radioactive biochemical assays (Millipore and Galapagos N.V.)) EUB0000626a TYK2	B	6.94	pIC50	116	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb	-	-	6.94	pIC50	116	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	Inhibition of recombinant human TYK2 using GGMEDIYFEFMGGKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method	B	6.95	pIC50	113	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
ChEMBL	Inhibition of recombinant TYK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay	B	6.95	pIC50	111.7	nM	IC50	J Med Chem (2023) 66: 16342-16363 [PMID:38031930]
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.06	pIC50	86.77	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.1	pIC50	79.07	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	TYK2 Inhibition Assay: Recombinant human TYK2 catalytic domain (amino acids 871-1187; catalog number 08-147) is purchased from Carna biosciences. 5 ng of TYK2 is incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (25 mM Hepes pH 7.5, 100 mM NaCl, 0.2 mM Na3VO4, 0.1% NP-40, 0.1 μM non-radioactive ATP, 0.125 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions are stopped by adding 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity is determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series are prepared for the compounds enabling the testing of dose-response effects in the TYK2 assay and the calculation of the IC50 for each compound. Each compound is routinely tested at concentration of 20 μM followed by a 1/3 serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions are prepared and/or the top concentration is lowered (e.g. 5 μM, 1 μM).	B	7.11	pIC50	78	nM	IC50	US-10919890-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.13	pIC50	73.75	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	TYK2 Inhibition Assay: Recombinant human TYK2 catalytic domain (amino acids 871-1187; catalog number 08-147) was purchased from Carna biosciences. 5 ng of TYK2 was incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (25 mM Hepes pH 7.5, 100 mM NaCl, 0.2 mM Na3VO4, 0.1% NP-40, 0.1 μM non-radioactive ATP, 0.125 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions were stopped by adding 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series were prepared for the compounds enabling the testing of dose-response effects in the TYK2 assay and the calculation of the IC50 for each compound. Each compound was routinely tested at concentration of 20 μM followed by a ⅓ serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions were prepared and/or the top concentration was lowered (e.g. 5 μM, 1 μM).	B	7.14	pIC50	72.7	nM	IC50	US-11000528-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.14	pIC50	72.7	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition of recombinant TYK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay	B	7.19	pIC50	65.3	nM	IC50	J Med Chem (2021) 64: 958-979 [PMID:33428419]
NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Obg-like ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Peroxisomal acyl-coenzyme A oxidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
phosphatidylinositol-5-phosphate 4-kinase type 2 alpha/Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795194] [GtoPdb: 2858] [UniProtKB: P48426]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Probable ATP-dependent RNA helicase DDX6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105783] [UniProtKB: P26196]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Putative heat shock protein HSP 90-beta 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Pyridoxal kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075181] [UniProtKB: O00764]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Ras-related C3 botulinum toxin substrate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6094] [UniProtKB: P63000]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Ras-related protein Rab-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105971] [UniProtKB: P61026]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Ras-related protein Rab-6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105703] [UniProtKB: P20340]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of human FLT3 (unknown origin)	B	6.47	pIC50	338	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Selectivity interaction (Radioactive biochemical assays (Millipore and Galapagos N.V.)) EUB0000626a FLT3	B	6.47	pIC50	338	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of Flt3 (unknown origin)	B	6.47	pIC50	338	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of ROCK1 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.72	pKd	1912	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Serine/threonine kinase 38 like/Serine/threonine-protein kinase 38-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4851] [GtoPdb: 1518] [UniProtKB: Q9Y2H1]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of ICK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
p21 (RAC1) activated kinase 6/Serine/threonine-protein kinase PAK 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4311] [GtoPdb: 2137] [UniProtKB: Q9NQU5]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of PAK6 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of TBK1 (unknown origin)	B	5.75	pIC50	1791	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Signal recognition particle receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105934] [UniProtKB: P08240]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.03	pKd	9273	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Structural maintenance of chromosomes protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Structural maintenance of chromosomes protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105890] [UniProtKB: O95347]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of ABL (unknown origin)	B	5.64	pIC50	2302	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of BTK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Selectivity interaction (Fluorescent competition binding assays) EUB0000626a JAK1@kinase 1	B	7.96	pKd	11	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Binding affinity to human recombinant JAK1 assessed as dissociation constant by Cheng-Prusoff equation analysis	B	7.96	pKd	11	nM	Kd	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	B	5.84	pIC50	1430	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
ChEMBL	Enzyme Inhibition Assay: Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino acids 831-1132, AstraZeneca R&D Boston), or JAK3 (amino acids 781-1124, AstraZeneca R&D Boston) under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 μg/ml BSA, and 10 mM MgCl2. JAK enzyme was expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes were assayed at their approximated high end of physiological ATP concentration of 5 mM, in the presence of inhibitor dosed at 30, 3, 0.3, 0.03, 0.003 and 0 μM final test concentrations.For JAK1, 4 nM of enzyme was incubated with 1.5 μM peptide substrate (FITC-C6-KKHTDDGYMPMSPGVA-NH2 (SEQ ID NO:1), Intonation, Boston, Mass.). For JAK2, 0.3 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2 (SEQ ID NO:2), Intonation, Boston, Mass.), For JAK3, 0.1 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NII2 (SEQ ID NO:2), Intonation, Boston, Mass.). Phosphorylated and unphosphotylated peptides were separated and quantified by a Caliper LC3000 system (Caliper Life Sciences, MA) for calculating percent inhibition.	B	6.09	pIC50	814	nM	IC50	US-10961228-B2. JAK1 selective inhibitors (2021)
ChEMBL	Inhibition of recombinant human JAK1 assessed as phosphorylation level in presence of 1 mM ATP	B	6.2	pIC50	636	nM	IC50	Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659]
ChEMBL	Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis	B	6.2	pIC50	629.51	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis	B	6.2	pIC50	629	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1 in human whole blood assessed as inhibition of IL-6-induced pSTAT1	B	6.2	pIC50	629	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK1 in human whole blood assessed as reduction in IL-6 induced STAT1 phosphorylation preincubated for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometer analysis	B	6.2	pIC50	629	nM	IC50	J Med Chem (2024) 67: 8545-8568 [PMID:38805213]
GtoPdb	-	-	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Inhibition of JAK1 (unknown origin)	B	6.44	pIC50	363	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Affinity Phenotypic Cellular interaction (Flow Cytometry (STAT6 phosphorylation induced by IL-4 in THP-1 cells)) EUB0000626a JAK1	F	6.75	pIC50	178	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of JAK1 signaling pathway in human THP-1 cells assessed as reduction in IL-4 induced STAT6 phosphorylation preincubated with compound for 1 hr followed by IL-4 addition and measured after 60 mins by flowcytometry analysis	B	6.75	pIC50	177.83	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1 signaling pathway in human THP-1 cells assessed as reduction in IL-4 induced STAT6 phosphorylation preincubated with compound for 1 hr followed by IL-4 addition and measured after 60 mins by flowcytometry analysis	B	6.81	pIC50	154	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK1 (unknown origin) in presence of ATP at Km concentration by caliper assay	B	6.94	pIC50	115	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
ChEMBL	JAK1 Inhibition Assay: Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) was purchased from Carna Biosciences. 10 ng of JAK1 was incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (15 mM Tris-HCl pH 7.5, 1 mM DTT, 0.01% Tween-20, 10 mM MgCl2, 2 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 45 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100%.	B	7	pIC50	<100	nM	IC50	US-10206907-B2. Compounds useful for the treatment of degenerative and inflammatory diseases (2019)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.25	pIC50	55.66	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	JAK1 Inhibition Assay: Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) is purchased from Carna Biosciences. 10 ng of JAK1 is incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (15 mM Tris-HCl pH 7.5, 1 mM DTT, 0.01% Tween-20, 10 mM MgCl2, 2 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 45 min at 30° C., reactions are stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity is determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series are prepared for the compounds enabling the testing of dose-response effects in the JAK1 assay and the calculation of the IC50 for each compound. Each compound is routinely tested at concentration of 20 μM followed by a 1/3 serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions are prepared and/or the top concentration is lowered (e.g. 5 μM, 1 μM).	B	7.3	pIC50	50.3	nM	IC50	US-10919890-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.3	pIC50	50.1	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition Assay: JAK1 (IC50): Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) is purchased from Carna Biosciences. 10 ng of JAK1 is incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (15 mM Tris-HCl pH 7.5, 1 mM DTT, 0.01% Tween-20, 10 mM MgCl2, 2 μM non-radioactive ATP, 0.25 μCi33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 pt, in a polypropylene 96-well plate (Greiner, V-bottom). After 45 min at 30° C., reactions are stopped by adding of 25 μL /well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle.	B	7.3	pIC50	50	nM	IC50	US-10708263-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2020)
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	7.3	pIC50	50	nM	IC50	US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	7.3	pIC50	50	nM	IC50	US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s).	B	7.3	pIC50	50	nM	IC50	US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.32	pIC50	48.29	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	JAK1 Inhibition Assay: Recombinant human JAK1 catalytic domain (amino acids 850-1154; catalog number 08-144) was purchased from Carna Biosciences. 10 ng of JAK1 was incubated with 12.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (15 mM Tris-HCl pH 7.5, 1 mM DTT, 0.01% Tween-20, 10 mM MgCl2, 2 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 45 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100. Dose dilution series were prepared for the compounds enabling the testing of dose-response effects in the JAK1 assay and the calculation of the IC50 for each compound. Each compound was routinely tested at concentration of 20 μM followed by a ⅓ serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions were prepared and/or the top concentration was lowered (e.g. 5 μM, 1 μM).	B	7.33	pIC50	47.1	nM	IC50	US-11000528-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.33	pIC50	47.07	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50.	B	7.34	pIC50	46	nM	IC50	US-11279699-B2. Compound as selective JAK inhibitor, and salt and therapeutic use thereof (2022)
ChEMBL	Inhibition of recombinant human JAK1 using MGEEPLYWSFPAKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method	B	7.48	pIC50	33	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
ChEMBL	Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay	B	7.58	pIC50	26.2	nM	IC50	J Med Chem (2021) 64: 958-979 [PMID:33428419]
ChEMBL	Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay	B	7.78	pIC50	16.5	nM	IC50	J Med Chem (2023) 66: 16342-16363 [PMID:38031930]
GtoPdb	-	-	7.96	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	Inhibition of recombinant JAK1 (unknown origin) in the presence of ATP	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL	Affinity Biochemical interaction (Radiometric kinase assay (incorporation of phosphate into an ULight-JAK-1(Tyr1023) peptide using an europium-labeled anti-phosphotyrosine Ab)) EUB0000626a JAK1	B	8	pIC50	10	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of JAK 1 (unknown origin)	B	8	pIC50	10	nM	IC50	J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL	Inhibition of human JAK1 using GEEPLYWSFPAKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method	B	8	pIC50	10	nM	IC50	Medchemcomm (2018) 9: 477-489 [PMID:30108938]
ChEMBL	Inhibition of JAK1 (unknown origin)	B	8	pIC50	10	nM	IC50	J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL	Inhibition of human recombinant JAK1 incubated for 60 mins	B	8	pIC50	10	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of human recombinant JAK1	B	8	pIC50	10	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK1 (unknown origin)	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL	Inhibition of recombinant human JAK1 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate preincubated with compound for 60 mins followed by substrate addition and measured after 90 mins in presence of ATP	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL	Selectivity interaction (Fluorescent competition binding assays) EUB0000626a JAK2	B	7.49	pKd	32	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Binding affinity to human recombinant JAK2 assessed as dissociation constant by Cheng-Prusoff equation analysis	B	7.49	pKd	32	nM	Kd	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis	B	4.76	pIC50	17458.22	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF induced STAT5 phosphorylation preincubated for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometer analysis	B	4.76	pIC50	17453	nM	IC50	J Med Chem (2024) 67: 8545-8568 [PMID:38805213]
ChEMBL	Inhibition of JAK2 in human whole blood assessed as inhibition of GM-CSF-induced pSTAT5	B	4.76	pIC50	17453	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis	B	4.76	pIC50	17453	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis	B	4.88	pIC50	13200	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5	B	5	pIC50	>10000	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK2 in EPO-induced human UT7-EPO cells assessed as pSTAT5	B	5	pIC50	>10000	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK2 signaling pathway in human 22Rv1 cells assessed as reduction in PRL-induced STAT5 phosphorylation incubated for 20 mins by Western blot analysis	B	5	pIC50	<10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 signaling pathway in human 22Rv1 cells assessed as reduction in PRL-induced STAT5 phosphorylation incubated for 20 mins by Western blot analysis	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 signaling pathway in human UT-7/Epo cells assessed as reduction in EPO-induced STAT5 phosphorylation preincubated with compound for 1 hr followed by EPO addition and measured after 20 mins by Alphascreen analysis	B	5	pIC50	<10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of JAK2 signaling pathway in human UT-7/Epo cells assessed as reduction in EPO-induced STAT5 phosphorylation preincubated with compound for 1 hr followed by EPO addition and measured after 20 mins by Alphascreen analysis	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Enzyme Inhibition Assay: Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino acids 831-1132, AstraZeneca R&D Boston), or JAK3 (amino acids 781-1124, AstraZeneca R&D Boston) under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 μg/ml BSA, and 10 mM MgCl2. JAK enzyme was expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes were assayed at their approximated high end of physiological ATP concentration of 5 mM, in the presence of inhibitor dosed at 30, 3, 0.3, 0.03, 0.003 and 0 μM final test concentrations.For JAK1, 4 nM of enzyme was incubated with 1.5 μM peptide substrate (FITC-C6-KKHTDDGYMPMSPGVA-NH2 (SEQ ID NO:1), Intonation, Boston, Mass.). For JAK2, 0.3 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2 (SEQ ID NO:2), Intonation, Boston, Mass.), For JAK3, 0.1 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NII2 (SEQ ID NO:2), Intonation, Boston, Mass.). Phosphorylated and unphosphotylated peptides were separated and quantified by a Caliper LC3000 system (Caliper Life Sciences, MA) for calculating percent inhibition.	B	5.17	pIC50	6770	nM	IC50	US-10961228-B2. JAK1 selective inhibitors (2021)
ChEMBL	Inhibition of JAK2 signalling in human whole blood assessed as inhibition of GM-CSF stimulated STAT5 phosphorylation in CD33+ monocytes preincubated for 1 hr followed by GM-CSF stimulation and incubated for 20 mins by flow cytometry analysis	B	5.27	pIC50	5333.3	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
ChEMBL	Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation	B	5.34	pIC50	4546	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	B	5.35	pIC50	4450	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
ChEMBL	Inhibition of JAK2 signaling pathway in human TF-1 cells assessed as reduction in IL-3-induced STAT5 phosphorylation preincubated with compound for 1 hr followed by IL-3 addition and measured after 20 mins by Alphascreen analysis	B	5.45	pIC50	3548.13	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Affinity Phenotypic Cellular interaction (AlphaScreen (STAT5 phosphorylation induced by IL-3 in TF-1 cells)) EUB0000626a JAK2	F	5.45	pIC50	3548	nM	IC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5	B	5.45	pIC50	3524	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of JAK2 signaling pathway in human TF-1 cells assessed as reduction in IL-3-induced STAT5 phosphorylation preincubated with compound for 1 hr followed by IL-3 addition and measured after 20 mins by Alphascreen analysis	B	5.45	pIC50	3524	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of recombinant human JAK2 assessed as phosphorylation level in presence of 1 mM ATP	B	5.62	pIC50	2400	nM	IC50	Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659]
ChEMBL	Inhibition of JAK2 (unknown origin)	B	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
GtoPdb	-	-	5.62	pIC50	2400	nM	IC50	J Med Chem (2014) 57: 5023-38 [PMID:24417533]
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	6.34	pIC50	460	nM	IC50	US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s).	B	6.34	pIC50	460	nM	IC50	US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	6.34	pIC50	460	nM	IC50	US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL	Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay	B	6.73	pIC50	184.9	nM	IC50	J Med Chem (2023) 66: 16342-16363 [PMID:38031930]
ChEMBL	Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay	B	6.77	pIC50	171	nM	IC50	J Med Chem (2021) 64: 958-979 [PMID:33428419]
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	6.78	pIC50	167.34	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition of recombinant human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method	B	6.91	pIC50	122	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
ChEMBL	JAK2 Inhibition Assay: Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) was purchased from Invitrogen. 0.025 mU of JAK2 was incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (5 mM MOPS pH 7.5, 9 mM MgAc, 0.3 mM EDTA, 0.06% Brij and 0.6 mM DTT, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100%.	B	7	pIC50	<100	nM	IC50	US-10206907-B2. Compounds useful for the treatment of degenerative and inflammatory diseases (2019)
ChEMBL	Inhibition of JAK2 (unknown origin) in presence of ATP at Km concentration by caliper assay	B	7.13	pIC50	74	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
ChEMBL	Enzyme Assay: JAK1 (KI): For the determination of Ki, different amounts of compound are mixed with the enzyme and the enzymatic reaction is followed as a function of ATP concentration. The Ki is determined by means of double reciprocal plotting of Km vs compound concentration (Lineweaver-Burk plot). 1 ng of JAK1 (Invitrogen, PV4774) is used in the assay. The substrate is 50 nM Ulight-JAK-1 (Tyr1023) Peptide (Perkin Elmer, TRF0121) The reaction is performed in 25 mM MOPS pH 6.8, 0.01%, 2 mM DTT, 5 mM MgCl2 Brij-35 with varying concentrations of ATP and compound. Phosphorylated substrate is measured using an Eu-labeled anti-phosphotyrosine antibody PT66 (Perkin Elmer, AD0068). Readout is performed on the envision (Perkin Elmer) with excitation at 320 nm and emission followed at 615 nm and 665 nm.	B	7.13	pIC50	74	nM	IC50	US-10708263-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2020)
ChEMBL	JAK2 Inhibition Assay: Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) is purchased from Invitrogen. 0.025 mU of JAK2 is incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (5 mM MOPS pH 7.5, 9 mM MgAc, 0.3 mM EDTA, 0.06% Brij and 0.6 mM DTT, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions are stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity is determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series are prepared for the compounds enabling the testing of dose-response effects in the JAK2 assay and the calculation of the IC50 for each compound. Each compound is routinely tested at concentration of 20 μM followed by a 1/3 serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions are prepared and/or the top concentration is lowered (e.g. 5 μM, 1 μM).	B	7.13	pIC50	73.4	nM	IC50	US-10919890-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.26	pIC50	55.49	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50.	B	7.26	pIC50	55	nM	IC50	US-11279699-B2. Compound as selective JAK inhibitor, and salt and therapeutic use thereof (2022)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.39	pIC50	41.16	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
GtoPdb	-	-	7.49	pIC50	28	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	JAK2 Inhibition Assay: Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) was purchased from Invitrogen. 0.025 mU of JAK2 was incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (5 mM MOPS pH 7.5, 9 mM MgAc, 0.3 mM EDTA, 0.06% Brij and 0.6 mM DTT, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prcwashcd (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series were prepared for the compounds enabling the testing of dose-response effects in the JAK2 assay and the calculation of the IC50 for each compound. Each compound was routinely tested at concentration of 20 μM followed by a ⅓ serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions were prepared and/or the top concentration was lowered (e.g. 5 μM, 1 μM).	B	7.5	pIC50	31.4	nM	IC50	US-11000528-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2021)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	7.5	pIC50	31.37	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition of recombinant human JAK2 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate preincubated with compound for 60 mins followed by substrate addition and measured after 90 mins in presence of ATP	B	7.55	pIC50	28	nM	IC50	Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL	Inhibition of recombinant JAK2 (unknown origin) in the presence of ATP	B	7.55	pIC50	28	nM	IC50	Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL	Affinity Biochemical interaction (Radiometric kinase assay (incorporation of phosphate into an ULight-JAK-1(Tyr1023) peptide using an europium-labeled anti-phosphotyrosine Ab)) EUB0000626a JAK2	B	7.55	pIC50	28	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of JAK2 (unknown origin)	B	7.55	pIC50	28	nM	IC50	Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL	Inhibition of JAK 2 (unknown origin)	B	7.55	pIC50	28	nM	IC50	J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL	Inhibition of JAK2 (unknown origin)	B	7.6	pIC50	25	nM	IC50	J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL	Inhibition of human recombinant JAK2 incubated for 60 mins	B	7.6	pIC50	25	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL	Selectivity interaction (Fluorescent competition binding assays) EUB0000626a JAK3	B	6.52	pKd	300	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Binding affinity to human recombinant JAK3 assessed as dissociation constant by Cheng-Prusoff equation analysis	B	6.52	pKd	300	nM	Kd	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Enzyme Inhibition Assay: Enzyme inhibition studies were performed using recombinant JAK1 (amino acids 866-1154, Life Technologies, #PV4774, Carlsbad, Calif.), JAK2 (amino acids 831-1132, AstraZeneca R&D Boston), or JAK3 (amino acids 781-1124, AstraZeneca R&D Boston) under buffer conditions of 50 mM HEPES pH 7.3, 1 mM DTT, 0.01% Tween-20, 50 μg/ml BSA, and 10 mM MgCl2. JAK enzyme was expressed as N-terminal GST fusion in insect cells and purified by glutathione-affinity and size-exclusion chromatographies. Enzymes were assayed at their approximated high end of physiological ATP concentration of 5 mM, in the presence of inhibitor dosed at 30, 3, 0.3, 0.03, 0.003 and 0 μM final test concentrations.For JAK1, 4 nM of enzyme was incubated with 1.5 μM peptide substrate (FITC-C6-KKHTDDGYMPMSPGVA-NH2 (SEQ ID NO:1), Intonation, Boston, Mass.). For JAK2, 0.3 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NH2 (SEQ ID NO:2), Intonation, Boston, Mass.), For JAK3, 0.1 nM enzyme was incubated with 1.5 μM peptide substrate (5FAM-GEEPLYWSFPAKKK-NII2 (SEQ ID NO:2), Intonation, Boston, Mass.). Phosphorylated and unphosphotylated peptides were separated and quantified by a Caliper LC3000 system (Caliper Life Sciences, MA) for calculating percent inhibition.	B	4.52	pIC50	>30000	nM	IC50	US-10961228-B2. JAK1 selective inhibitors (2021)
ChEMBL	Inhibition of JAK3 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	B	4.88	pIC50	13260	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
ChEMBL	Inhibition of JAK3 (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Med Chem (2014) 57: 5023-5038 [PMID:24417533]
ChEMBL	Inhibition of recombinant human JAK3 assessed as phosphorylation level in presence of 1 mM ATP	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem Lett (2021) 38: 127862-127862 [PMID:33609659]
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	5.03	pIC50	9400	nM	IC50	US-10766894-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2020)
ChEMBL	Kinase Assay: A kinase selectivity panel which measures substrate peptide phosphorylation was set-up for recombinant human Jak1 (aa 866-1154), Jak2 (aa808-1132), Jak3 (aa811-1124) and Tyk2 (aa888-1187). The technology used for the described assay is based on the separation and quantification of substrate and product in an electrical field. In the course of the kinase reaction the peptide substrate is phosphorylated by a kinase. The transfer of a phosphate residue also causes the introduction of two additional negative charges and hence to a change in the net charge of the phospho-peptide compared to the unphosphorylated peptide. Due to this difference in charge the phosphorylated und unphosphorylated peptides migrate with different velocities in an electrical field.In the applied method, this separation takes place inside a chip that contains a complex capillary system for simultaneous analysis of 12 samples (12-sipper chip, Caliper Technologies Corp., Mountain View, USA). In order to allow the detection and quantification of the peptides in the capillary system, the peptides carry a fluorescent label (fluorescein). With this label the peptides can be quantified by fluorescence intensity through the instruments laser and detection system (LC3000, Caliper Life Sciences).The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ß-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.Plates with terminated kinase reactions were transferred to the Caliper LC3000 workstation (Caliper Technologies Corp., Mountain View, USA) for reading. The relative amount of phosphorylated peptide r, was calculated using the heights of the substrate peak, s, and the product peak, p: r=p/(p+s).	B	5.03	pIC50	9400	nM	IC50	US-10112907-B2. Substituted indazoles for treating tendon and/or ligament injuries (2018)
ChEMBL	Biochemical Activity Assay: The assays were performed in 384-well, low volume microtiter assay plates in a final reaction volume of 9 ul. Dose-response curves were generated by incubating 3 nM of each kinase together with 2 uM of a fluorescently labeled substrate peptide specific for each enzyme (Jak1 and Jak3 substrate FITC-Ahx-KKSRGDYMTMQIG-NH2, Jak2 and Tyk2 substrate 5(6)-Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK) in 50 mM Hepes pH 7.5, 0.02% Tween 20, 0.02% BSA, 1 mM DTT, 10 uM Na3VO4, 10 mM ��-Glycerolphosphate, specific concentrations of MgCl2 (Jak1 12 mM, Jak2 and Tyk2 9 mM, Jak3 1.5 mM) and 45 uM ATP for 60 min at 30° C. in the presence or absence of compound diluted in DMSO. Kinase reaction were terminated by adding 15 ul STOP buffer (100 mM HEPES pH 7.5, 5% DMSO, 0.1% Caliper coating reagent, 10 mM EDTA, and 0.015% Brij35.	B	5.03	pIC50	9400	nM	IC50	US-11203595-B2. Aza-indazole compounds for use in tendon and/or ligament injuries (2021)
ChEMBL	Inhibition of recombinant human JAK3 using GGEEEEYFELVKKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method	B	5.51	pIC50	3083	nM	IC50	J Med Chem (2022) 65: 16716-16740 [PMID:36512734]
ChEMBL	Inhibition of recombinant JAK3 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay	B	6.03	pIC50	932	nM	IC50	J Med Chem (2021) 64: 958-979 [PMID:33428419]
ChEMBL	Inhibition of recombinant human JAK3 using ULight-JAK-1(Tyr1023) peptide as substrate assessed as incorporation of phosphate into the substrate preincubated with compound for 60 mins followed by substrate addition and measured after 90 mins in presence of ATP	B	6.09	pIC50	810	nM	IC50	Eur J Med Chem (2022) 239: 114551-114551 [PMID:35749986]
ChEMBL	Inhibition of JAK3 (unknown origin)	B	6.09	pIC50	810	nM	IC50	J Med Chem (2015) 58: 7596-7602 [PMID:26351728]
ChEMBL	Inhibition of human JAK3 using GGEEEEYFELVKKKK as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method	B	6.09	pIC50	810	nM	IC50	Medchemcomm (2018) 9: 477-489 [PMID:30108938]
ChEMBL	Inhibition of recombinant JAK3 (unknown origin) in the presence of ATP	B	6.09	pIC50	810	nM	IC50	Eur J Med Chem (2020) 192: 112155-112155 [PMID:32120325]
ChEMBL	Inhibition of JAK3 (unknown origin)	B	6.09	pIC50	810	nM	IC50	Eur J Med Chem (2023) 261: 115848-115848 [PMID:37793326]
ChEMBL	Inhibition of human recombinant JAK3 incubated for 60 mins	B	6.09	pIC50	810	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition of recombinant JAK3 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay	B	6.18	pIC50	653.6	nM	IC50	J Med Chem (2023) 66: 16342-16363 [PMID:38031930]
ChEMBL	Inhibition of JAK: The study of the effect of compounds on the activity of purified recombinant JAK was performed by studying the inhibitory activity of the compounds on JAK from the enzymatic level. The experimental principle is to use a luminescence kinase assay to detect the ADP content produced by the reaction of JAK with the substrate Poly (4:1 Glu, Tyr) peptide: after ADP is converted to ATP, ATP can act as a substrate for the Ultra-Glo luciferase catalytic reaction, producing an optical signal. The luminescence signal is positively correlated with the amount of ADP and kinase activity. Therefore, the inhibitory effect of the compounds on the recombinant JAK was determined by observing the luminescence signal produced by the reaction of JAK and the substrate, and was expressed by IC50.	B	6.19	pIC50	644	nM	IC50	US-11279699-B2. Compound as selective JAK inhibitor, and salt and therapeutic use thereof (2022)
ChEMBL	Inhibition of JAK3 (unknown origin) in presence of ATP at Km concentration by caliper assay	B	6.21	pIC50	623	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127225-127225 [PMID:32527540]
GtoPdb	-	-	6.52	pIC50	810	nM	IC50	J Immunol (2013) 191: 3568-77 [PMID:24006460]
ChEMBL	Inhibition of JAK3 signaling pathway in human THP-1 cells assessed as reduction in IL-4 induced STAT6 phosphorylation preincubated with compound for 1 hr followed by IL-4 addition and measured after 60 mins by flowcytometry analysis	B	6.69	pIC50	203	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	6.71	pIC50	194.7	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	6.72	pIC50	189.3	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	6.73	pIC50	187.3	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	JAK3 Inhibition Assay: Recombinant human JAK3 catalytic domain (amino acids 781-1124; catalog number PV3855) is purchased from Invitrogen. 0.025 mU of JAK3 is incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (25 mM Tris pH 7.5, 0.5 mM EGTA, 0.5 mM Na3VO4, 5 mM b-glycerolphosphate, 0.01% Triton X-100, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 105 min at 30° C., reactions are stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity is determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series are prepared for the compounds enabling the testing of dose-response effects in the JAK3 assay and the calculation of the IC50 for each compound. Each compound is routinely tested at concentration of 20 μM followed by a 1/3 serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions are prepared and/or the top concentration is lowered (e.g. 5 μM, 1 μM).	B	6.74	pIC50	180	nM	IC50	US-10919890-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2021)
ChEMBL	Inhibition Assay: JAK2 (IC50): Recombinant human JAK2 catalytic domain (amino acids 808-1132; catalog number PV4210) is purchased from Invitrogen. 0.025 mU of JAK2 is incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (5 mM MOPS pH 7.5, 9 mM MgAc, 0.3 mM EDTA, 0.06% Brij and 0.6 mM DTT, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 90 min at 30° C., reactions are stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction is transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates are washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates is sealed. 40 μL/well of Microscint-20 is added, the top of the plates is sealed and readout is performed using the Topcount (Perkin Elmer). Kinase activity is calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle.	B	6.74	pIC50	180	nM	IC50	US-10708263-B2. Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders (2020)
ChEMBL	Inhibition Assay: In vitro inhibition assay using various enzyme.	B	6.83	pIC50	149.35	nM	IC50	US-8563545-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2013)
ChEMBL	JAK3 Inhibition Assay: Recombinant human JAK3 catalytic domain (amino acids 781-1124; catalog number PV3855) was purchased from Invitrogen. 0.025 mU of JAK3 was incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (25 mM Tris pH 7.5, 0.5 mM EGTA, 0.5 mM Na3VO4, 5 mM b-glycerolphosphate, 0.01% Triton X-100, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 105 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100.Dose dilution series were prepared for the compounds enabling the testing of dose-response effects in the JAK3 assay and the calculation of the IC50 for each compound. Each compound was routinely tested at concentration of 20 μM followed by a ⅓ serial dilution, 8 points (20 μM-6.67 μM-2.22 μM-740 nM-247 nM-82 nM-27 nM-9 nM) in a final concentration of 1% DMSO. When potency of compound series increased, more dilutions were prepared and/or the top concentration was lowered (e.g. 5 μM, 1 μM).	B	6.83	pIC50	149	nM	IC50	US-11000528-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2021)
ChEMBL	JAK3 Inhibition Assay: Recombinant human JAK3 catalytic domain (amino acids 781-1124; catalog number PV3855) was purchased from Invitrogen. 0.025 mU of JAK3 was incubated with 2.5 μg polyGT substrate (Sigma catalog number P0275) in kinase reaction buffer (25 mM Tris pH 7.5, 0.5 mM EGTA, 0.5 mM Na3VO4, 5 mM b-glycerophosphate, 0.01% Triton X-100, 1 μM non-radioactive ATP, 0.25 μCi 33P-gamma-ATP (GE Healthcare, catalog number AH9968) final concentrations) with or without 5 μL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 25 μL, in a polypropylene 96-well plate (Greiner, V-bottom). After 105 min at 30° C., reactions were stopped by adding of 25 μL/well of 150 mM phosphoric acid. All of the terminated kinase reaction was transferred to prewashed (75 mM phosphoric acid) 96 well filter plates (Perkin Elmer catalog number 6005177) using a cell harvester (Perkin Elmer). Plates were washed 6 times with 300 μL per well of a 75 mM phosphoric acid solution and the bottom of the plates was sealed. 40 μL/well of Microscint-20 was added, the top of the plates was sealed and readout was performed using the Topcount (Perkin Elmer). Kinase activity was calculated by subtracting counts per minute (cpm) obtained in the presence of a positive control inhibitor (10 μM staurosporine) from cpm obtained in the presence of vehicle. The ability of a test compound to inhibit this activity was determined as:Percentage inhibition=((cpm determined for sample with test compound present−cpm determined for sample with positive control inhibitor) divided by (cpm determined in the presence of vehicle−cpm determined for sample with positive control inhibitor))*100%.	B	7	pIC50	<100	nM	IC50	US-10206907-B2. Compounds useful for the treatment of degenerative and inflammatory diseases (2019)
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of LCK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of LYNA (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
ChEMBL	Inhibition of Mer (unknown origin)	B	5.89	pIC50	1274	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
ChEMBL	Inhibition of SYK (unknown origin)	B	5	pIC50	>10000	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Tyrosine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
UMP-CMP kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5681] [UniProtKB: P30085]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	5.36	pKd	4384	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL	Inhibition of Flt1 (unknown origin)	B	5.88	pIC50	1327	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL	Inhibition of human FLT4 (unknown origin)	B	6.56	pIC50	274	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Selectivity interaction (Radioactive biochemical assays (Millipore and Galapagos N.V.)) EUB0000626a FLT4	B	6.56	pIC50	274	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of Flt4 (unknown origin)	B	6.56	pIC50	274	nM	IC50	J Immunol (2013) 191: 3568-3577 [PMID:24006460]
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105892] [UniProtKB: P49748]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG channel by patch clamp assay	B	4	pIC50	>100000	nM	IC50	J Med Chem (2014) 57: 9323-9342 [PMID:25369270]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells by automated patch clamp method	B	4.07	pIC50	85000	nM	IC50	Bioorg Med Chem (2018) 26: 1495-1510 [PMID:29452839]
ChEMBL	Inhibition of human ERG expressed in HEK293 cells after 5 mins by automated planar patch clamp method	B	4.07	pIC50	85000	nM	IC50	Medchemcomm (2018) 9: 477-489 [PMID:30108938]
WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291]
ChEMBL	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	B	4.52	pKd	>30000	nM	Kd	Science (2017) 358: null-null [PMID:29191878]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]