etavopivat [Ligand Id: 11975] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL4650332 (Etavopivat, Ft-4202, FT-4202)
  • Probable ubiquitin carboxyl-terminal hydrolase FAF-X in Human [ChEMBL: CHEMBL2406899] [UniProtKB: Q93008]
There should be some charts here, you may need to enable JavaScript!
  • pyruvate kinase L/R in Human [GtoPdb: 3007] [UniProtKB: P30613]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Probable ubiquitin carboxyl-terminal hydrolase FAF-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2406899] [UniProtKB: Q93008]
ChEMBL Inhibition of USP9X (unknown origin) using Ubiquitin-Rhoadmine 110 as substrate preincubated for 30 mins followed by substrate addition and measured after 11 mins by fluorescence assay B 5.7 pIC50 2000 nM IC50 WO-2020061261-A1. Inhibiting ubiquitin specific peptidase 9x (null)
pyruvate kinase L/R in Human [GtoPdb: 3007] [UniProtKB: P30613]
GtoPdb Activation of wild-type PKR by etavopivat in mature, purified human RBCs - 6.95 pEC50 113 nM EC50 J Pharmacol Exp Ther (2022) 380: 210-219 [PMID:35031585]

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]