L-45 [Ligand Id: 11703] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4570969
  • lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831]
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  • Plasmodium falciparum histone acetyltransferase GCN5 in Plasmodium falciparum [GtoPdb: 3191]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831]
ChEMBL Binding affinity to human PCAF bromodomain by isothermal titration calorimetry B 6.9 pKd 126 nM Kd J Med Chem (2019) 62: 4526-4542 [PMID:30998845]
ChEMBL Inhibition of biotinylated peptide binding to human GST-tagged PCAF bromodomain expressed in Escherichia coli Rosetta (DE3) measured after 15 hrs by HTRF assay B 7.44 pIC50 36 nM IC50 J Med Chem (2019) 62: 4526-4542 [PMID:30998845]
Plasmodium falciparum histone acetyltransferase GCN5 in Plasmodium falciparum [GtoPdb: 3191]
GtoPdb Isothermal titration calorimetry. - 6.55 pKd 280 nM Kd Angew Chem Int Ed Engl (2017) 56: 827-831 [PMID:27966810]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]