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ChEMBL ligand: CHEMBL505121 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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 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 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 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 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 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]