TAK-632 [Ligand Id: 10387] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3125890 |
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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: P20248, P24941] | ||||||||
| 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: P06493, P14635] | ||||||||
| 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 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
| ChEMBL | Inhibition of human wild type RIPK1 (M1 to K305) expressed in bacterial system by kinomescan assay | B | 6.32 | pKd | 480 | nM | Kd | Bioorg Med Chem Lett (2021) 43: 128084-128084 [PMID:33964444] |
| GtoPdb | Binding constant determined by KINOMEscan assay. | - | 6.32 | pKd | 480 | nM | Kd | Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190] |
| 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] |
| ChEMBL | Inhibition of human wild type RIPK3 (M1 to Q307) expressed in bacterial system by kinomescan assay | B | 6.98 | pKd | 105 | nM | Kd | Bioorg Med Chem Lett (2021) 43: 128084-128084 [PMID:33964444] |
| 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] |
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]
