altiratinib [Ligand Id: 9174] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3545365 (Altiratinib, DCC-2701, DP-5164) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 MET (unknown origin) | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| ChEMBL | Inhibition of c-MET (unknown origin) | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2018) 158: 814-831 [PMID:30248654] |
| ChEMBL | Inhibition of cMET (unknown origin) | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| GtoPdb | - | - | 8.57 | pIC50 | 2.7 | nM | IC50 | WO2016061231. Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression (2016) |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Inhibition of TrkA (unknown origin) | B | 9.07 | pIC50 | 0.85 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| ChEMBL | Inhibition of TRKA (unknown origin) | B | 9.07 | pIC50 | 0.85 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of TrkB (unknown origin) | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| ChEMBL | Inhibition of TRKB (unknown origin) | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| ChEMBL | Inhibition of TRKC (unknown origin) | B | 8.08 | pIC50 | 8.3 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| ChEMBL | Inhibition of TrkC (unknown origin) | B | 9.08 | pIC50 | 0.83 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Inhibition of TIE-2 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| ChEMBL | Inhibition of TIE2 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| GtoPdb | - | - | 8.62 | pIC50 | 2.4 | nM | IC50 | WO2016061231. Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression (2016) |
| 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) | B | 8.04 | pIC50 | 9.2 | nM | IC50 | Eur J Med Chem (2018) 158: 814-831 [PMID:30248654] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) | B | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2019) 62: 1731-1760 [PMID:30188734] |
| GtoPdb | - | - | 8.04 | pIC50 | 9.2 | nM | IC50 | WO2016061231. Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression (2016) |
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]
