compound 20 [PMID: 22136433] [Ligand Id: 8156] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1945559
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • calcium/calmodulin-dependent protein kinase II beta subunit/CaM kinase II beta in Human [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
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  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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  • EPH receptor A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
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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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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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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 activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
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  • phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • protein kinase C theta/Protein kinase C theta in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
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  • protein kinase N1/Protein kinase N1 in Human [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
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  • protein kinase N2/Protein kinase N2 in Human [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
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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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  • WNK lysine deficient protein kinase 1/Serine/threonine-protein kinase WNK1 in Human [ChEMBL: CHEMBL1075173] [GtoPdb: 2280] [UniProtKB: Q9H4A3]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
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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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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947]
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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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  • Calmodulin-dependent kinase II in Human [GtoPdb: 1554]
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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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
calcium/calmodulin-dependent protein kinase II beta subunit/CaM kinase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
ChEMBL Inhibition of CaMK2 using ATP as substrate B 7.08 pIC50 83 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CK1alpha using ATP as substrate B 6.48 pIC50 330 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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/D1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of recombinant CLK3 (unknown origin) using Ac-ERMRPRKRQGSVdP(Sox)G-NH2 as substrate after 5 mins by Omnia Kinase Assay B 4.57 pKi 26900 nM Ki J Med Chem (2020) 63: 10224-10234 [PMID:32787076]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of full length wild type CLK1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay B 6.85 pKi 140 nM Ki J Med Chem (2020) 63: 10224-10234 [PMID:32787076]
EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
ChEMBL Inhibition of EphA4 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL Inhibition of EphB4 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of HER1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of FGFR2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Inhibition of FGFR3 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
ChEMBL Inhibition of FGFR3 kinase domain using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Inhibition of FGFR4 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of FAK using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 cMET using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of IGF1R using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of Ins1R using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 Inhibition of IRAK4 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Inhibition of RON using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 MK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Inhibition of MK5 using ATP as substrate B 5.77 pIC50 1700 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279]
ChEMBL Inhibition of COT1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9]
ChEMBL Inhibition of VPS34 using ATP as substrate B 5.04 pIC50 >9100 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Inhibition of PI3Kalpha using ATP as substrate B 5.04 pIC50 >9100 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
ChEMBL Inhibition of PI3Kbeta using ATP as substrate B 5.07 pIC50 8600 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Inhibition of PI3Kdelta using ATP as substrate B 5.33 pIC50 4700 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of PI3Kgamma using ATP as substrate B 5.51 pIC50 3100 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
phosphatidylinositol 4-kinase beta/PI4-kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8]
ChEMBL Inhibition of PI4Kbeta using ATP as substrate B 5.6 pIC50 2500 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of PDGFRalpha using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of PKCalpha using ATP as substrate B 5.66 pIC50 2200 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Inhibition of PKCtheta using ATP as substrate B 5.85 pIC50 1400 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
protein kinase N1/Protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512]
ChEMBL Inhibition of PKN1 using ATP as substrate B 6.51 pIC50 310 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
GtoPdb - - 6.51 pIC50 310 nM IC50 J Med Chem (2012) 55: 403-13 [PMID:22136433]
protein kinase N2/Protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513]
ChEMBL Inhibition of PKN2 using ATP as substrate B 6.52 pIC50 300 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of HER2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
ChEMBL Inhibition of HER4 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 Inhibition of ROCK2 using ATP as substrate B 6.66 pIC50 220 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 PKBalpha using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of Aurora A using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of mTOR using ATP as substrate B 5.04 pIC50 >9100 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177]
ChEMBL Inhibition of PAK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
GtoPdb - - 7.22 pIC50 60 nM IC50 J Med Chem (2012) 55: 403-13 [PMID:22136433]
ChEMBL Inhibition of PIM1 using ATP as substrate B 7.22 pIC50 60 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 6.62 pIC50 240 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
ChEMBL Inhibition of PIM3 using ATP as substrate B 7.05 pIC50 90 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
GtoPdb - - 7.05 pIC50 90 nM IC50 J Med Chem (2012) 55: 403-13 [PMID:22136433]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
WNK lysine deficient protein kinase 1/Serine/threonine-protein kinase WNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075173] [GtoPdb: 2280] [UniProtKB: Q9H4A3]
ChEMBL Inhibition of WNK1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 cKIT using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 cABL using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
ChEMBL Inhibition of cABL T315I mutant using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Inhibition of CSK using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of FYN using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Inhibition of HCK using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of JAK1 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET using ATP as substrate B 5.11 pIC50 7700 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of AXL using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of cSRC using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of SYK using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Inhibition of TYK2 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 Inhibition of YES using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 using ATP as substrate B 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
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 KDR using ATP as substrate B 5.14 pIC50 7200 nM IC50 J Med Chem (2012) 55: 403-413 [PMID:22136433]
Calmodulin-dependent kinase II in Human [GtoPdb: 1554]
GtoPdb - - 7.08 pIC50 83 nM IC50 J Med Chem (2012) 55: 403-13 [PMID:22136433]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]