ChEMBL ligand: CHEMBL1215739
lysine acetyltransferase 5/Histone acetyltransferase KAT5 in Human [ChEMBL: CHEMBL5750] [GtoPdb: 2664] [UniProtKB: Q92993] There should be some charts here, you may need to enable JavaScript!
lysine acetyltransferase 8/Histone acetyltransferase KAT8 in Human [ChEMBL: CHEMBL1932912] [GtoPdb: 2668] [UniProtKB: Q9H7Z6] There should be some charts here, you may need to enable JavaScript!
E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] There should be some charts here, you may need to enable JavaScript!

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 N-terminal 6His tagged KAT8 (173 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using biotinylated histone H4 peptide and [3H]Acetyl-CoA as substrates preincubated for 20 mins followed by substrate addition and measured after 4 hrs by MicroBeta microplate counter analysis	B	4.69	pIC50	20300	nM	IC50	J Med Chem (2023) 66: 6591-6616 [PMID:37155735]
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]
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Inhibition of recombinant human KAT3B (1287 to 1673 residues) using histone H3 peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis	B	4.65	pIC50	22300	nM	IC50	J Med Chem (2023) 66: 6591-6616 [PMID:37155735]

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]