compound A127 [WO2013110309] [Ligand Id: 8169] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3260333
  • eukaryotic translation initiation factor 2 alpha kinase 4/Eukaryotic translation initiation factor 2-alpha kinase 4 in Human [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8]
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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 4/Eukaryotic translation initiation factor 2-alpha kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5358] [GtoPdb: 2018] [UniProtKB: Q9P2K8]
GtoPdb - - 6.52 pIC50 300 nM IC50 ACS Med Chem Lett (2014) 5: 282-3 [PMID:24900825]
ChEMBL Inhibition of GCN2 (unknown origin) using GFP-elF2a as substrate preincubated with substrate for 20 mins measured after 90 mins by Lanthascreen assay B 6.52 pIC50 <300 nM IC50 ACS Med Chem Lett (2014) 5: 282-283 [PMID:24900825]
ChEMBL Inhibition of GCN2-mediated elF2alpha phosphorylation in human U2OS cells after 2 hrs by immunocytochemistry B 6.52 pIC50 300 nM IC50 ACS Med Chem Lett (2014) 5: 282-283 [PMID:24900825]

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]