mevrometostat [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 Y641N mutant (unknown origin) B 10 pKi <0.1 nM Ki Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]