A-366 [Ligand Id: 8238] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3109630
  • 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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  • euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
GtoPdb - - 8.48 pIC50 3.3 nM IC50 A-366: a chemical Probe for G9a/GLP.. thesgc.org;
ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801]
ChEMBL Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assay B 8.48 pIC50 3.3 nM IC50 ACS Med. Chem. Lett. (2014) 5: 205-209 [PMID:24900801]
ChEMBL Inhibition of G9a (unknown origin) B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2015) 58: 2569-2583 [PMID:25406944]
ChEMBL Inhibition of G9a (unknown origin) B 8.48 pIC50 3.3 nM IC50 Bioorg Med Chem (2016) 24: 6102-6108 [PMID:27720557]
ChEMBL Inhibition of G9a (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay B 8.52 pIC50 3 nM IC50 ACS Med. Chem. Lett. (2014) 5: 205-209 [PMID:24900801]
euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1]
ChEMBL Inhibition of GLP (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay B 7.42 pIC50 38 nM IC50 ACS Med. Chem. Lett. (2014) 5: 205-209 [PMID:24900801]
GtoPdb - - 8.52 pIC50 38 nM IC50 A-366: a chemical Probe for G9a/GLP.. thesgc.org;
ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]