valemetostat [Ligand Id: 12282] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4597193 (Valemetostat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Inhibition of wildtype EZH1 (unknown origin) | B | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2023) 256: 115461-115461 [PMID:37156182] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | Cancer Sci (2017) 108: 2069-2078 [PMID:28741798] |
| ChEMBL | Inhibition of human EZH1 by radiometric analysis | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Eur J Med Chem (2023) 256: 115461-115461 [PMID:37156182] |
| ChEMBL | Inhibition of EZH1 (unknown origin) | B | 9.36 | pIC50 | 0.44 | nM | IC50 | J Med Chem (2022) 65: 7016-7043 [PMID:35531606] |
| 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] | ||||||||
| ChEMBL | Inhibition of EZH2 (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2023) 256: 115461-115461 [PMID:37156182] |
| ChEMBL | Inhibition of EZH2 (unknown origin) assessed as reduction in H3K27me3 level | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2022) 65: 7016-7043 [PMID:35531606] |
| GtoPdb | - | - | 8.29 | pIC50 | 5.1 | nM | IC50 | Cancer Sci (2017) 108: 2069-2078 [PMID:28741798] |
| ChEMBL | Inhibition of EZH2 (unknown origin) | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2022) 65: 7016-7043 [PMID:35531606] |
| ChEMBL | Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Eur J Med Chem (2023) 256: 115461-115461 [PMID:37156182] |
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]
