HC-5404 [Ligand Id: 13275] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4862478
  • eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
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  • Eukaryotic translation initiation factor 2 subunit 1 in Human [ChEMBL: CHEMBL1255131] [UniProtKB: P05198]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5]
ChEMBL Inhibition of human His-tagged PERK expressed in Escherichia coli assessed as eIF2alpha phosphorylation by TR-FRET assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2021) 43: 128058-128058 [PMID:33895276]
GtoPdb Inhibition of human His-tagged PERK by measuring eIF2alpha phosphorylation in a TR-FRET assay - 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2021) 43: 128058 [PMID:33895276]
Eukaryotic translation initiation factor 2 subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1255131] [UniProtKB: P05198]
ChEMBL Inhibition of eIF2alpha (unknown origin) assessed as eIF2alpha phosphorylation by TR-FRET assay B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2021) 43: 128058-128058 [PMID:33895276]

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]