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 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]
