rodatristat [Ligand Id: 10647] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4104957 (KAR5417, Rodatristat, RVT-1201/014)
  • L-Tryptophan hydroxylase 1/Tryptophan 5-hydroxylase 1 in Human [ChEMBL: CHEMBL5689] [GtoPdb: 1241] [UniProtKB: P17752]
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  • L-Tryptophan hydroxylase 2 in Human [GtoPdb: 1242] [UniProtKB: Q8IWU9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
L-Tryptophan hydroxylase 1/Tryptophan 5-hydroxylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5689] [GtoPdb: 1241] [UniProtKB: P17752]
GtoPdb - - 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2017) 27: 413-419 [PMID:28041831]
ChEMBL Inhibition of TPH1 (unknown origin) B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2017) 27: 413-419 [PMID:28041831]
L-Tryptophan hydroxylase 2 in Human [GtoPdb: 1242] [UniProtKB: Q8IWU9]
GtoPdb - - 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2017) 27: 413-419 [PMID:28041831]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]