azacitidine [Ligand Id: 6796] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1489 (Vidaza, NSC-102816, U-18496, Azacitidine, Ladakamycin)
  • DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
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  • euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358]
ChEMBL Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay B 6.52 pIC50 300 nM IC50 J Med Chem (2018) 61: 6518-6545 [PMID:29953809]
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
ChEMBL Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 6518-6545 [PMID:29953809]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]