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)
  • tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
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  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612]
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  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II subunit alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • 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: O00311, Q9UBU7]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418]
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  • eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • High affinity immunoglobulin gamma Fc receptor I in Human [ChEMBL: CHEMBL5349] [UniProtKB: P12314]
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  • neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
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  • mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683]
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  • tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • protein kinase C beta/Protein kinase C beta type in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882]
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  • ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
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  • pyruvate dehydrogenase kinase 1/[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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  • AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
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  • NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98]
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  • serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84]
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  • p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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  • tousled like kinase 2/Serine/threonine-protein kinase tousled-like 2 in Human [ChEMBL: CHEMBL5404] [GtoPdb: 2243] [UniProtKB: Q86UE8]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
tyrosine kinase non receptor 2/Activated CDC42 kinase 1 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]
ChEMBL Inhibition of ACK1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of ALK (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
aurora kinase A/Aurora kinase 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/Aurora kinase 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]
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 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 subunit 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: O00311, Q9UBU7]
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]
ChEMBL Inhibition of CDC7/DBF4 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
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]
ChEMBL Inhibition of CDK1/CycB (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
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: P24864, P24941]
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]
ChEMBL Inhibition of CDK2/CycE (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
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]
ChEMBL Inhibition of CDK4/CycD1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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]
ChEMBL Inhibition of CDK5/P25 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of EphA2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase 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]
ChEMBL Inhibition of EEF2K (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of PERK (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of FGFR1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of GSK3beta (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of MET (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor 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]
ChEMBL Inhibition of TRKA (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
IGF-like family receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2029192] [UniProtKB: Q9H665]
ChEMBL Inhibition of IGFR1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta 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]
ChEMBL Inhibition of IKK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of IR (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of MAPKAPK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 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 Inhibition of MNK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 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]
ChEMBL Inhibition of KIT (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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
ChEMBL Inhibition of MELK (unknown origin) in presence of [gamma-33P]ATP B 6.13 pIC50 744 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 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]
ChEMBL Inhibition of ERK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 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]
ChEMBL Inhibition of P38alpha (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of BUB1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
tyrosine kinase 2/Non-receptor 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]
ChEMBL Inhibition of TYK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
protein kinase C beta/Protein kinase C beta type 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]
ChEMBL Inhibition of PKC beta (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
protein tyrosine kinase 6/Protein-tyrosine kinase 6 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]
ChEMBL Inhibition of BRK (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
ret proto-oncogene/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]
ChEMBL Inhibition of RET (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of ROS (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
pyruvate dehydrogenase kinase 1/[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial 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]
ChEMBL Inhibition of PDK1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase 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]
ChEMBL Inhibition of AKT1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase 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
ChEMBL Inhibition of FLT3 (unknown origin) in presence of [gamma-33P]ATP B 6.29 pIC50 510 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 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]
ChEMBL Inhibition of MST4 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of CHK1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of Haspin (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of NEK6 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of NIM1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of PAK4 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 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]
ChEMBL Inhibition of PIM1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 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]
ChEMBL Inhibition of PIM2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Binding affinity to PLK1 (unknown origin) assessed as inhibition constant incubated for 180 mins in presence of [gamma-33P]ATP B 8.8 pKi 1.58 nM Ki Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of PLK1 (unknown origin) in presence of [gamma-33P]ATP B 8.7 pIC50 2 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of PLK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of PLK3 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of TLK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
Small ribosomal subunit protein eS27 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1932893] [UniProtKB: P42677]
ChEMBL Inhibition of MPS1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 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]
ChEMBL Inhibition of ABL (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of JAK1 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of JAK3 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of LCK (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of LYN (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of SYK (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of ZAP70 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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]
ChEMBL Inhibition of VEGFR2 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]
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 Inhibition of VEGFR3 (unknown origin) in presence of [gamma-33P]ATP B 5 pIC50 >10000 nM IC50 Mol Cancer Ther (2012) 11: 1006-1016 [PMID:22319201]

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]