PF-06821497 [Ligand Id: 10516] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4080228 (Pf-06821497, PF-06821497)
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  • enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800]
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  • enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 650-665 [PMID:29211475]
enhancer of zeste 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800]
ChEMBL Binding affinity to EZH1 (unknown origin) B 7.15 pKi 70 nM Ki J Med Chem (2018) 61: 650-665 [PMID:29211475]
enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910]
GtoPdb Inhibition of enzyme function in a biochemical assay using the (activating) Y641N mutant form of EZH2. - 10 pKi <0.1 nM Ki J Med Chem (2018) 61: 650-665 [PMID:29211475]
ChEMBL Inhibition of EZH2 Y641N mutant (unknown origin) using oligonucleosomes as substrate after 60 mins in presence of [3H]SAM by scintillation counting analysis B 10 pKi <0.1 nM Ki J Med Chem (2018) 61: 650-665 [PMID:29211475]
ChEMBL Binding affinity to EZH2 (unknown origin) B 10 pKi <0.1 nM Ki J Med Chem (2018) 61: 650-665 [PMID:29211475]
ChEMBL Inhibition of EZH2 in human KARPAS422 cells assessed as reduction in H3K27me3 level after 72 hrs by ELISA B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 650-665 [PMID:29211475]

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]