TAK-632 [Ligand Id: 10387] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3125890
  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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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 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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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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  • 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]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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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 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • Platelet-derived growth factor subunit A in Human [ChEMBL: CHEMBL3137294] [UniProtKB: P04085]
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  • protein kinase C theta/Protein kinase C theta in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
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  • receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
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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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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
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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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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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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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  • receptor interacting serine/threonine kinase 1 in Human [GtoPdb: 2189] [UniProtKB: Q13546]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta (unknown origin) using CK1tide as substrate after 20 mins B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248P24941]
ChEMBL Inhibition of CDK2/CycA (unknown origin) using histone H1 as substrate after 20 mins B 6.24 pIC50 580 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibition of C-terminal FLAG-tagged JNK1 (unknown origin) expressed in baculovirus system using c-jun as substrate after 60 mins B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 (unknown origin) using histone H1 as substrate after 20 mins B 6.1 pIC50 790 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Inhibition of N-terminal GST-tagged MEK1 (unknown origin) expressed in 293 cells using GST-ERK1(K71A) as substrate after 20 mins B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL In Vitro Inhibition Assay: MEK phosphorylation inhibition activity. B 6.52 pIC50 <300 nM IC50 US-8497274-B2. Heterocyclic compound and use thereof (2013)
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of N-terminal peptide (DYKDDDD)-tagged EGFR (unknown origin) expressed in baculovirus system using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs by scintillation counting B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
GtoPdb Biochemical enzyme inhibition assay. - 6.55 pIC50 280 nM IC50 J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of FGFR3 (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 6.55 pIC50 280 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 C-terminal FLAG-tagged GSK3beta (unknown origin) expressed in baculovirus system after 30 mins B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
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 c-Met receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 C-terminal FLAG-tagged IKK beta (unknown origin) expressed in baculovirus system using IkappaBalpha as substrate after 40 mins B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of Insulin receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of C-terminal FLAG-tagged ERK1 expressed in baculovirus system (unknown origin) using MBP as substrate after 60 mins B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of C-terminal FLAG-tagged p38 alpha (unknown origin) expressed in baculovirus system using MBP as substrate after 60 mins B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
ChEMBL Inhibition of C-terminal FLAG-tagged MEKK1 (unknown origin) expressed in baculovirus system using MBP as substrate after 60 mins B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
Pirin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010627] [UniProtKB: O00625]
ChEMBL Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb Biochemical enzyme inhibition assay. - 6.92 pIC50 120 nM IC50 J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of PDGFR beta (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 6.92 pIC50 120 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
Platelet-derived growth factor subunit A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3137294] [UniProtKB: P04085]
ChEMBL Inhibition of PDGFR alpha (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 6.21 pIC50 610 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL Inhibition of C-terminal FLAG-tagged PKC-theta (unknown origin) expressed in Escherichia coli using MBP as substrate after 60 mins B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL Binding affinity to wild-type human partial length RIPK3 (M1 to Q307 residues) expressed in bacterial expression system after 1 hr by quantitative PCR based KINOMEscan assay B 6.98 pKd 105 nM Kd J Med Chem (2019) 62: 6665-6681 [PMID:31095385]
GtoPdb Binding constant determined by KINOMEscan assay. - 6.98 pKd 105 nM Kd Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190]
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 N-terminal peptide (DYKDDDD)-tagged HER2 (unknown origin) expressed in baculovirus system using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs by scintillation counting B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
GtoPdb Biochemical enzyme inhibition assay. - 7.18 pIC50 66 nM IC50 J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of N-terminal His-6-tagged Aurora kinase B (unknown origin) expressed in baculovirus system after 60 mins B 7.18 pIC50 66 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
GtoPdb Dissociation constant determined using Surface Plasmon Resonance. - 8.8 pKd 1.6 nM Kd J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of recombinant wild type full length human GST-tagged B-Raf expressed in baculovirus expression system using Z'-LYTE Ser/Thr3 peptide as substrate incubated for 1 hr by FRET-based Z'-LYTE assay B 7.11 pIC50 77 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2760-2763 [PMID:27155899]
ChEMBL Inhibition of BRAF V600E mutant in human HT-29 cells assessed as phosphorylation of MEK B 7.12 pIC50 75 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of BRAF V600E mutant (unknown origin) in presence of 1000 uM ATP by ELISA B 7.24 pIC50 58 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Competitive inhibition of BRAF V600E mutant (unknown origin) in presence of 5 uM ATP by ELISA B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged B-Raf V600E mutant expressed in baculovirus expression system using Z'-LYTE Ser/Thr3 peptide as substrate incubated for 1 hr by FRET-based Z'-LYTE assay B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2760-2763 [PMID:27155899]
ChEMBL Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
GtoPdb Biochemical enzyme inhibition assay. - 8.08 pIC50 8.3 nM IC50 J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of N-terminal FLAG-tagged wild type BRAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 mins B 8.08 pIC50 8.3 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system B 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
ChEMBL Inhibition of N-terminal 6x-His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 using C-terminal His-tagged/N-terminal GST-tagged full length human MEK1 as substrate after 1 hr by ELISA B 8.35 pIC50 4.48 nM IC50 J Med Chem (2018) 61: 5034-5046 [PMID:29727562]
ChEMBL Inhibition of BRAF V600E mutant (unknown origin) compound preincubated for 1 hr in presence of 1000 uM ATP B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of N-terminal 6x-His-tagged BRAF kinase domain (unknown origin) expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 using C-terminal His-tagged/N-terminal GST-tagged full length human MEK1 as substrate after 1 hr by ELISA B 8.49 pIC50 3.23 nM IC50 J Med Chem (2018) 61: 5034-5046 [PMID:29727562]
ChEMBL Inhibition of N-terminal FLAG-tagged recombinant BRAF V600E mutant (unknown origin) expressed in baculovirus system preincubated for 10 mins before substrate addition measured after 20 mins by scintillation counting B 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of BRAF V600E mutant (unknown origin) compound preincubated for 1 hr in presence of 5 uM ATP B 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression system B 8.7 pIC50 2 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of CHK1 (unknown origin) using alpha-casein as substrate after 20 mins B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
GtoPdb Dissociation constant determined by Surface Plasmon Resonance. - 9.28 pKd 0.52 nM Kd J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of CRAF (unknown origin) in presence of 1000 uM ATP by ELISA B 7.21 pIC50 62 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Competitive inhibition of CRAF (unknown origin) in presence of 0.5 uM ATP by ELISA B 8.09 pIC50 8.1 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of CRAF (unknown origin) compound preincubated for 1 hr in presence of 1000 uM ATP B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL Inhibition of CRAF (unknown origin) compound preincubated for 1 hr in presence of 0.5 uM ATP B 8.82 pIC50 1.5 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
GtoPdb Biochemical enzyme inhibition assay. - 8.85 pIC50 1.4 nM IC50 J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL Inhibition of N-terminal FLAG-tagged wild type C-RAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 mins B 8.85 pIC50 1.4 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 c-Kit receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 Src receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of TIE2 receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs B 6.13 pIC50 740 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
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 (unknown origin) using biotinylated poly-GluTyr (4:1) as substrate pretreated for 5 mins before substrate addition measured after overnight incubation B 6.8 pIC50 160 nM IC50 J. Med. Chem. (2013) 56: 6478-6494 [PMID:23906342]
receptor interacting serine/threonine kinase 1 in Human [GtoPdb: 2189] [UniProtKB: Q13546]
GtoPdb Binding constant determined by KINOMEscan assay. - 6.32 pKd 480 nM Kd Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]