bemcentinib [Ligand Id: 10478] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3809489 (Bemcentinib, BGB 324, BGB-324, BGB324, CS-1046, HY-15150, KB-80319, QC-11751, R 428, R-428, R428, SYN-1131, SYN1131, W-5845) |
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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 wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] | ||||||||
| ChEMBL | Inhibition of wild-type human partial length DDR1 (R565 to V876 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length MET (D1010 to S1367 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length PDGFRA (V575 to D1002 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Inhibition of human recombinant MER by fluorescence polarization assay | B | 6.15 | pIC50 | >700 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| ChEMBL | Inhibition of wild-type human partial length MER (R557 to L884 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 AKT (unknown origin) using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of human partial length Aurora A (E122 to K401 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Inhibition of wild-type human partial length AURKB (D25 to A303 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length MTOR (L1382 to W2549 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length KIT (I571 to D952 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 human recombinant ABL by fluorescence polarization assay | B | 6.15 | pIC50 | >700 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| 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 human partial length FLT3 ITD mutant expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| ChEMBL | Inhibition of human partial length FLT3 D835Y mutant (Q580 to Y969 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| ChEMBL | Inhibition of wild-type human partial length FLT3 (V592 to Y969 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of wild-type human partial length RET (E713 to D1014 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418] | ||||||||
| ChEMBL | Inhibition of human recombinant TYRO3 by fluorescence polarization assay | B | 6.15 | pIC50 | >700 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| ChEMBL | Inhibition of wild-type human partial length TYRO3 (S497 to T814 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA | B | 7.52 | pIC50 | <30 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | Cancer Res (2010) 70: 1544-54 [PMID:20145120] |
| ChEMBL | Inhibition of human recombinant AXL by fluorescence polarization assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2016) 59: 3593-3608 [PMID:26555154] |
| ChEMBL | Inhibition of AXL (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2021) 220: 113497-113497 [PMID:33957388] |
| ChEMBL | Inhibition of Axl (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2016) 59: 6807-6825 [PMID:27379978] |
| ChEMBL | Inhibition of AXL (unknown origin) by ELISA | B | 8.28 | pIC50 | 5.3 | nM | IC50 | Eur J Med Chem (2021) 220: 113497-113497 [PMID:33957388] |
| ChEMBL | Inhibition of human recombinant AXL incubated for 1 to 1.5 hrs by FRET based Z'-Lyte kinase assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2016) 59: 6807-6825 [PMID:27379978] |
| ChEMBL | Inhibition of wild-type human partial length AXL (R497 to Y821 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length SRC (L240 to L536 residues) expressed in bacterial expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
| 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 wild-type human partial length VEGFR2 (R787 to P1253 residues) expressed in mammalian expression system using poly [Glu, Try] 4:1 as substrate in presence of [gamma-33P]ATP | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2018) 61: 2104-2110 [PMID:29466002] |
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]
