onvansertib [Ligand Id: 7918] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1738758 (Nms-1286937, NMS-1286937, NMS-P937, Onvansertib, PCM-075)
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
Created with Highcharts 10.3.3ValuesChart context menuALK tyrosine kinase receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
Created with Highcharts 10.3.3ValuesChart context menucAMP-dependent protein kinase alpha-catalytic subunitpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
Created with Highcharts 10.3.3ValuesChart context menuCasein kinase II alphapKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311Q9UBU7]
Created with Highcharts 10.3.3ValuesChart context menuCDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase)pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 1/cyclin B1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 2/cyclin ApKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 2/cyclin E1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 4/cyclin D1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 5/CDK5 activator 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
Created with Highcharts 10.3.3ValuesChart context menuDual specificity protein kinase TTKpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
Created with Highcharts 10.3.3ValuesChart context menuEphrin type-A receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
Created with Highcharts 10.3.3ValuesChart context menuEukaryotic translation initiation factor 2-alpha kinase 3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
Created with Highcharts 10.3.3ValuesChart context menuFocal adhesion kinase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
Created with Highcharts 10.3.3ValuesChart context menuGlycogen synthase kinase-3 betapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
Created with Highcharts 10.3.3ValuesChart context menuHepatocyte growth factor receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • High affinity immunoglobulin gamma Fc receptor I in Human [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
Created with Highcharts 10.3.3ValuesChart context menuHigh affinity immunoglobulin gamma Fc receptor IpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
Created with Highcharts 10.3.3ValuesChart context menuInhibitor of nuclear factor kappa B kinase beta subunitpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuInsulin receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase-activated protein kinase 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase ERK2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase p38 alphapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
Created with Highcharts 10.3.3ValuesChart context menuMAP kinase signal-integrating kinase 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
Created with Highcharts 10.3.3ValuesChart context menuMaternal embryonic leucine zipper kinasepKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683]
Created with Highcharts 10.3.3ValuesChart context menuMitotic checkpoint serine/threonine-protein kinase BUB1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
Created with Highcharts 10.3.3ValuesChart context menuNerve growth factor receptor Trk-ApKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • protein kinase C beta/Protein kinase C beta in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
Created with Highcharts 10.3.3ValuesChart context menuProtein kinase C betapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
Created with Highcharts 10.3.3ValuesChart context menuProto-oncogene tyrosine-protein kinase ROSpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
Created with Highcharts 10.3.3ValuesChart context menuPyruvate dehydrogenase kinase isoform 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase AKTpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase Aurora-ApKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase Aurora-BpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase Chk1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • eukaryotic elongation factor 2 kinase/Serine/threonine-protein kinase EEF2K in Human [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase EEF2KpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase haspinpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase MST4pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase NEK6pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase NIM1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PAK 4pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PIM1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PIM2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PLK1pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PLK2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase PLK3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8]
Created with Highcharts 10.3.3ValuesChart context menuSerine/threonine-protein kinase tousled-like 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
Created with Highcharts 10.3.3ValuesChart context menuStem cell growth factor receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine kinase non-receptor protein 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase ABLpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase BRKpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase JAK1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase JAK3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase LCKpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase LynpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor FLT3pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor RETpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase SYKpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase TYK2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase ZAP-70pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
Created with Highcharts 10.3.3ValuesChart context menuVascular endothelial growth factor receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
Created with Highcharts 10.3.3ValuesChart context menuVascular endothelial growth factor receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of ALK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase alpha-catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
ChEMBL Inhibition of PKAalpha assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
ChEMBL Selectivity interaction (Kinase panel (radiometric kinase assay)) EUB0000677a CSNK2A1 B 6.08 pIC50 826 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311Q9UBU7]
ChEMBL Inhibition of CDC7/DBF4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of CDK1/CYCB assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of CDK2/CYCA assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of CDK2/CYCE assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/CYCD1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of CDK5/P25 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL Inhibition of MPS1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EphA2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
ChEMBL Inhibition of PERK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of FAK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of MET assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
High affinity immunoglobulin gamma Fc receptor I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
ChEMBL Inhibition of IGFR1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of IR assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of MAPKAPK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of P38alpha assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Inhibition of MNK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL Inhibition of MELK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 6.13 pIC50 744 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
ChEMBL Selectivity interaction (Kinase panel (radiometric kinase assay)) EUB0000677a MELK B 6.13 pIC50 744 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Inhibition of BUB1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of TRKA assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of PKCbeta assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL Inhibition of ROS1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
ChEMBL Inhibition of PDK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of Aur-A assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aur-B assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
eukaryotic elongation factor 2 kinase/Serine/threonine-protein kinase EEF2K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
ChEMBL Inhibition of EEF2K assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
ChEMBL Inhibition of Haspin assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Inhibition of MST4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
ChEMBL Inhibition of NEK6 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
ChEMBL Inhibition of NIM1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
ChEMBL Inhibition of PAK4 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of PIM1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL Inhibition of PIM2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Affinity Phenotypic Cellular interaction (Antiproliferative effect on A2780 cells) EUB0000677a PLK1 F 7.38 pIC50 42 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-gamma-ATP, and in the presence of their own optimal buffer and cofactors.At the end of the phosphorylation reaction, more than 98% cold ATP and radioactive ATP is captured by an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity.Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, then evaluated by beta-counting.Reagents/Assay Conditions i. Dowex Resin Preparation500 g of wet resin (SIGMA, custom prepared resin DOWEX 1x8 200-400 mesh, 2.5 Kg) are weighed out and diluted to 2 L in 150 mM sodium formate, pH 3.00.The resin is allowed to settle down. B 8.52 pIC50 3 nM IC50 US-8614220-B2. Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors (2013)
ChEMBL Inhibition of PLK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
ChEMBL Affinity Biochemical interaction (Radiometric kinase assay) EUB0000677a PLK1 B 8.7 pIC50 2 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of PLK1 (unknown origin) by ATP competitive assay B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2023) 251: 115242-115242 [PMID:36889251]
GtoPdb - - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862]
polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
GtoPdb - - 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862]
ChEMBL Inhibition of PLK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
GtoPdb - - 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862]
ChEMBL Inhibition of PLK3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8]
ChEMBL Inhibition of TLK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of KIT assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Inhibition of ACK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
ChEMBL Inhibition of BRK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of LYN assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb - - 6.29 pIC50 510 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-74 [PMID:21470862]
ChEMBL Inhibition of FLT3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 6.29 pIC50 510 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
ChEMBL Selectivity interaction (Kinase panel (radiometric kinase assay)) EUB0000677a FLT3 B 6.29 pIC50 510 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of Syk assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of TYK2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Inhibition of ZAP70 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]
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 VEGFR3 assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2969-2974 [PMID:21470862]

ChEMBL data shown on this page come from version 35:

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]