tulmimetostat [Ligand Id: 12615] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5095231 (Cpi 0209, CPI-0209, CPI0209, Tulmimetostat)
  • enhancer of zeste 2 polycomb repressive complex 2 subunit in Human [GtoPdb: 2654] [UniProtKB: Q15910]
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  • enhancer of zeste 1 polycomb repressive complex 2 subunit in Human [GtoPdb: 2835] [UniProtKB: Q92800]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
enhancer of zeste 2 polycomb repressive complex 2 subunit in Human [GtoPdb: 2654] [UniProtKB: Q15910]
GtoPdb Binding inhibition constant for EZH2 - 10.96 pKi 0.01 nM Ki US20220257577A1. Ezh2 inhibition in combination therapies for the treatment of cancers (2022)
GtoPdb Inhibition of catalytic activity of wild-type EZH2-containing PRC2 complex in a biochemical assay - 10.7 pIC50 0.02 nM IC50 US20220257577A1. Ezh2 inhibition in combination therapies for the treatment of cancers (2022)
enhancer of zeste 1 polycomb repressive complex 2 subunit in Human [GtoPdb: 2835] [UniProtKB: Q92800]
GtoPdb Inhibition of catalytic activity of wild-type EZH1-containing PRC2 complex in a biochemical assay - 10.22 pIC50 0.06 nM IC50 US20220257577A1. Ezh2 inhibition in combination therapies for the treatment of cancers (2022)

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]