altiratinib [Ligand Id: 9174] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3545365 (Altiratinib, DCC-2701, DP-5164)
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
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  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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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 32:

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]