C646 [Ligand Id: 7004] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1797936
  • E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
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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 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 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 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]