MG149 [Ligand Id: 7488] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1215739
  • lysine acetyltransferase 5/Histone acetyltransferase KAT5 in Human [ChEMBL: CHEMBL5750] [GtoPdb: 2664] [UniProtKB: Q92993]
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  • lysine acetyltransferase 8/Histone acetyltransferase KAT8 in Human [ChEMBL: CHEMBL1932912] [GtoPdb: 2668] [UniProtKB: Q9H7Z6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
lysine acetyltransferase 5/Histone acetyltransferase KAT5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5750] [GtoPdb: 2664] [UniProtKB: Q92993]
ChEMBL Competitive inhibition of human recombinant His-tagged Tip60 expressed in Escherichia coli BL21(DE3) cells by Michaelis-Menten equation in presence of Acetyl CoA B 3.24 pKi 572 uM Kii Eur J Med Chem (2012) 47: 337-344 [PMID:22100137]
ChEMBL Uncompetitive inhibition of human recombinant His-tagged Tip60 expressed in Escherichia coli BL21(DE3) cells by Michaelis-Menten equation in presence of peptide substrate H4 B 4.11 pKi 78 uM Kii Eur J Med Chem (2012) 47: 337-344 [PMID:22100137]
GtoPdb - - 4.13 pIC50 74000 nM IC50 Eur J Med Chem (2012) 47: 337-44 [PMID:22100137]
ChEMBL Inhibition of human recombinant His-tagged Tip60 expressed in Escherichia coli BL21(DE3) cells using [14C]Ac-AoA and histone H4 as substrate after 5 mins by scintillation counting B 4.13 pIC50 74000 nM IC50 Eur J Med Chem (2012) 47: 337-344 [PMID:22100137]
lysine acetyltransferase 8/Histone acetyltransferase KAT8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1932912] [GtoPdb: 2668] [UniProtKB: Q9H7Z6]
ChEMBL Inhibition of human MOF expressed in Escherichia coli BL21(DE3) cells using [14C]AC-CoA and histone H4 as substrate after 5 mins by scintillation counting B 4.33 pIC50 47000 nM IC50 Eur J Med Chem (2012) 47: 337-344 [PMID:22100137]
GtoPdb - - 4.33 pIC50 47000 nM IC50 Eur J Med Chem (2012) 47: 337-44 [PMID:22100137]
ChEMBL Inhibition of human His-tagged MOF preincubated for 10 mins followed by biotin-labeled H4K16 substrate addition measured after 30 mins in presence of acetyl-CoA by alphascreen assay B 4.57 pIC50 27000 nM IC50 Eur J Med Chem (2018) 157: 867-876 [PMID:30145373]
ChEMBL Inhibition of human His-tagged MOF using histone H4 substrate by radioactive acetylation assay B 4.82 pIC50 15000 nM IC50 Eur J Med Chem (2018) 157: 867-876 [PMID:30145373]

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]