ChEMBL ligand: CHEMBL505121
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!
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!
lysine acetyltransferase 2B in Human [GtoPdb: 2737] [UniProtKB: Q92831] 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	Inhibition of recombinant Tip60 (1-513) expressed in Escherichia coli BL21 (DE3) by liquid scintillation	B	4.53	pIC50	29750	nM	IC50	Bioorg Med Chem (2009) 17: 1381-1386 [PMID:19114310]
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Inhibition of p300 (unknown origin)	B	7.72	pKi	19	nM	Ki	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of recombinant p300	B	6.01	pIC50	980	nM	IC50	Bioorg Med Chem (2009) 17: 1381-1386 [PMID:19114310]
GtoPdb	-	-	6.3	pIC50	500	nM	IC50	Mol Cell (2000) 5: 589-95 [PMID:10882143]
ChEMBL	Inhibition of full length recombinant human FLAG-tagged p300 expressed in baculovirus expression system using histone substrate incubated for 10 mins by radiometric gel assay	B	6.3	pIC50	500	nM	IC50	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
ChEMBL	Inhibition of recombinant p300 (unknown origin) using mixed histones and acetyl-coA as substrates incubated for 10 mins	B	6.3	pIC50	500	nM	IC50	Eur J Med Chem (2022) 237: 114407-114407 [PMID:35512565]
ChEMBL	Inhibition of recombinant human p300 using [14C]acetyl-CoA as substrate measured after 10 mins by phosphor imaging analysis	B	6.3	pIC50	500	nM	IC50	J Med Chem (2020) 63: 1337-1360 [PMID:31910017]
ChEMBL	Inhibition of N-terminal His-tagged human recombinant p300 catalytic domain (1284-1673 residues) using histone H4-8 peptide and [14C]acetyl CoA as substrate pretreated with enzyme and H4-8 peptide for 10 mins followed by [14C]acetyl CoA addition for 5 to 10 mins by phosphor-imaging analysis	B	6.3	pIC50	500	nM	IC50	J Med Chem (2020) 63: 4716-4731 [PMID:32314924]
ChEMBL	Inhibition of recombinant FLAG-tagged human P300 expressed in Baculovirus expression system using histone peptide as substrate after 10 mins in presence of [14C]-acetyl CoA by phosphorimaging analysis	B	6.3	pIC50	500	nM	IC50	Bioorg Med Chem (2018) 26: 5397-5407 [PMID:30297119]
ChEMBL	Inhibition of recombinant full length p300 (unknown origin) using N-terminal H4-20 peptide substrate incubated for 7 mins by radiometric gel assay in presence of [14C]acetyl-CoA	B	7.3	pIC50	50	nM	IC50	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
ChEMBL	Inhibition of human recombinant C-terminal GST-tagged p300 (1195 to 1673 residues) expressed in competent Escherichia coli DH5alpha cells using histone substrate after 30 mins by scintillation counting method in presence of [3H]acetyl-CoA	B	8.49	pIC50	3.2	nM	IC50	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
lysine acetyltransferase 2B in Human [GtoPdb: 2737] [UniProtKB: Q92831]
GtoPdb	-	-	3.7	pIC50	200000	nM	IC50	Mol Cell (2000) 5: 589-95 [PMID:10882143]

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]