CH7057288 [Ligand Id: 12237] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4457566
  • 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 in Human [GtoPdb: 1818] [UniProtKB: Q16620]
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  • neurotrophic receptor tyrosine kinase 3 in Human [GtoPdb: 1819] [UniProtKB: Q16288]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 human TrkA G595R mutant expressed in mouse NIH/3T3 cells by HTRF assay B 7.08 pIC50 83 nM IC50 Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087]
ChEMBL Inhibition of human wild type TrkA kinase domain expressed in mouse NIH/3T3 cells by HTRF assay B 8.82 pIC50 1.5 nM IC50 Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087]
GtoPdb - - 8.92 pIC50 1.2 nM IC50 J Med Chem (2022) 65: 12427-12444 [PMID:36066182]
ChEMBL Inhibition of human TrkA G667C mutant expressed in mouse NIH/3T3 cells by HTRF assay B 9.17 pIC50 0.68 nM IC50 Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087]
neurotrophic receptor tyrosine kinase 2 in Human [GtoPdb: 1818] [UniProtKB: Q16620]
GtoPdb - - 8.7 pIC50 2 nM IC50 J Med Chem (2022) 65: 12427-12444 [PMID:36066182]
neurotrophic receptor tyrosine kinase 3 in Human [GtoPdb: 1819] [UniProtKB: Q16288]
GtoPdb - - 8.55 pIC50 2.8 nM IC50 J Med Chem (2022) 65: 12427-12444 [PMID:36066182]

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]