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 A2 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] |
| ChEMBL | Binding affinity to human wild type partial length RIPK1 (M1/Q307) expressed in bacterial expression system assessed as dissociation constant by biochemical assay | B | 6.32 | pKd | 480 | nM | Kd | J Med Chem (2023) 66: 2361-2385 [PMID:36781172] |
| ChEMBL | Binding affinity to recombinant RIPK1 (unknown origin) assessed as dissociation constant incubated for 1 hr by KINOMEscanTM assay | B | 6.32 | pKd | 480 | nM | Kd | J Med Chem (2023) 66: 15288-15308 [PMID:37917221] |
| GtoPdb | Binding constant determined by KINOMEscan assay. | - | 6.32 | pKd | 480 | nM | Kd | Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190] |
| ChEMBL | Binding affinity to RIPK1 (unknown origin) by ADP-GlO assay | B | 6.98 | pKd | 105 | nM | Kd | J Med Chem (2023) 66: 2361-2385 [PMID:36781172] |
| 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 human wild type partial length RIPK3 (M1/Q307) expressed in bacterial expression system assessed as dissociation constant by biochemical assay | B | 6.49 | pKd | 326 | nM | Kd | J Med Chem (2023) 66: 2361-2385 [PMID:36781172] |
| 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] |
| ChEMBL | Binding affinity to recombinant RIPK3 (unknown origin) assessed as dissociation constant incubated for 1 hr by KINOMEscanTM assay | B | 6.98 | pKd | 105 | nM | Kd | J Med Chem (2023) 66: 15288-15308 [PMID:37917221] |
| GtoPdb | Binding constant determined by KINOMEscan assay. | - | 6.98 | pKd | 105 | nM | Kd | Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190] |
| ChEMBL | Inhibition of human RIPK3 using MBP as substrate by [gamma33-ATP] based radiometric assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2023) 66: 2361-2385 [PMID:36781172] |
| 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 | 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 | 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 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 human full length wild type B-Raf | B | 8.08 | pIC50 | 8.3 | nM | IC50 | Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788] |
| 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 B-Raf V600E mutant (unknown origin) | B | 8.62 | pIC50 | 2.4 | nM | IC50 | Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788] |
| 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 34:
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]
