example 203 [WO2017058503A1] [Ligand Id: 12664] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4587289
  • SUV39H2 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H2 in Human [ChEMBL: CHEMBL1795177] [GtoPdb: 2716] [UniProtKB: Q9H5I1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
SUV39H2 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795177] [GtoPdb: 2716] [UniProtKB: Q9H5I1]
GtoPdb Inhibition of SUV39H2-mediated H3 histone peptide methylation using [3H]-SAM as the methyl donor - 8.75 pIC50 1.77 nM IC50 WO2017058503A1. Bicyclic compound and use thereof for inhibiting suv39h2 (2017)
ChEMBL Inhibition of SUV39H2 (unknown origin) using H3 histone peptide substrate and [3H]-SAM incubated for 3 hrs by microbeta counting based assay B 8.75 pIC50 1.77 nM IC50 US-20180273529-A1. Bicyclic compound and use thereof for inhibiting suv39h2 (null)

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]