L-45 [Ligand Id: 11703] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4570969 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| lysine acetyltransferase 2A/Histone acetyltransferase GCN5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5501] [GtoPdb: 2736] [UniProtKB: Q92830] | ||||||||
| ChEMBL | Affinity On-target Cellular interaction (Competing pull-down assay (full-length GCN5 from cell lysates using immobilized L-Moses)) EUB0000218c KAT2A | B | 6.66 | pIC50 | 220 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Biochemical interaction (BROMOscan assay (DiscoverX)) EUB0000218c KAT2A | B | 6.66 | pIC50 | 220 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] | ||||||||
| ChEMBL | Binding affinity to human PCAF bromodomain by isothermal titration calorimetry | B | 6.9 | pKd | 126 | nM | Kd | J Med Chem (2019) 62: 4526-4542 [PMID:30998845] |
| ChEMBL | Affinity On-target Cellular interaction (Competing pull-down assay (full-length PCAF from cell lysates using immobilized L-Moses)) EUB0000218c KAT2B | B | 6.18 | pIC50 | 660 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Affinity Biochemical interaction (BROMOscan assay (DiscoverX)) EUB0000218c KAT2B | B | 7.32 | pIC50 | 48 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of biotinylated peptide binding to human GST-tagged PCAF bromodomain expressed in Escherichia coli Rosetta (DE3) measured after 15 hrs by HTRF assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2019) 62: 4526-4542 [PMID:30998845] |
| Plasmodium falciparum histone acetyltransferase GCN5 in Plasmodium falciparum [GtoPdb: 3191] | ||||||||
| GtoPdb | Isothermal titration calorimetry. | - | 6.55 | pKd | 280 | nM | Kd | Angew Chem Int Ed Engl (2017) 56: 827-831 [PMID:27966810] |
ChEMBL data shown on this page come from version 35:
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]
