pinometostat [Ligand Id: 7019] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3087499 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3] | ||||||||
| GtoPdb | - | - | 10.1 | pKi | 0.08 | nM | Ki | Blood (2013) 122: 1017-25 [PMID:23801631] |
| ChEMBL | Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor | B | 10.15 | pKi | <0.07 | nM | Ki | J Med Chem (2013) 56: 8972-8983 [PMID:23879463] |
| ChEMBL | Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assay | B | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2013) 56: 8972-8983 [PMID:23879463] |
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]
