ChEMBL ligand: CHEMBL1797936
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
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Competitive inhibition of p300 HAT	B	6.4	pKi	400	nM	Ki	Bioorg Med Chem (2011) 19: 3605-3615 [PMID:21316248]
ChEMBL	Competitive inhibition of p300 (unknown origin) using acetyl CoA as substrate	B	6.4	pKi	400	nM	Ki	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA	B	6.4	pKi	400	nM	Ki	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
GtoPdb	-	-	6.4	pKi	400	nM	Ki	Chem Biol (2010) 17: 471-82 [PMID:20534345]
ChEMBL	Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of DTT and BSA	B	4.29	pIC50	51000	nM	IC50	ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290]
ChEMBL	Inhibition of EP300 (unknown origin) by AlphaLISA immunodetection assay	B	4.3	pIC50	>50000	nM	IC50	Bioorg Med Chem Lett (2021) 51: 128358-128358 [PMID:34534674]
ChEMBL	Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of DTT	B	4.89	pIC50	13000	nM	IC50	ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290]
ChEMBL	Inhibition of FLAG-tagged p300 (1195 to 1673 residues) (unknown origin) expressed in competent Escherichia coli BL21-CodonPlus(DE3)-RIL cells using histone H4 substrate incubated for 10 mins by scintillation counting method in presence of [14C]acetyl-CoA	B	5.05	pIC50	9000	nM	IC50	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
ChEMBL	Inhibition of recombinant P300 catalytic domain (1284 to 1673 residues) (unknown origin) using FITC- histone H4 peptide (1 to 19 residues) as substrate by electrophoretic mobility shift assay	B	5.17	pIC50	6800	nM	IC50	ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290]
ChEMBL	Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of BSA	B	5.7	pIC50	2000	nM	IC50	ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290]
ChEMBL	Inhibition of VMA intein chitin binding domain-fused P300 (unknown origin) (1287 to 1652 residues) expressed in Escherichia coli BL21(RIL)-DE3 cells using [12C]-acetyl-CoA/[14C]-acetyl-CoA as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by phosphor imaging analysis	B	5.8	pIC50	1600	nM	IC50	J Med Chem (2020) 63: 1337-1360 [PMID:31910017]
ChEMBL	Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA	B	5.8	pIC50	1600	nM	IC50	J Med Chem (2016) 59: 1249-1270 [PMID:26701186]
ChEMBL	Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis	B	6	pIC50	1000	nM	IC50	ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290]
ChEMBL	Inhibition of p300 (unknown origin)	B	6.4	pIC50	400	nM	IC50	Eur J Med Chem (2019) 180: 171-190 [PMID:31306905]
ChEMBL	Inhibition of p300 (unknown origin) using biotinylated histone H3 (1 to 21 residues) as substrate measured after 90 mins in presence of Acetyl CoA by AlphaLISA assay	B	6.64	pIC50	230	nM	IC50	Eur J Med Chem (2019) 180: 171-190 [PMID:31306905]

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]