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ChEMBL ligand: CHEMBL5095231 (Cpi 0209, CPI-0209, CPI0209, Tulmimetostat) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]