Assay Detail
Binding
CHEMBL4153627
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Inhibition of yeast GCN5 (99 to 262 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 15 mins followed by biotin tagged H3 peptide ( 1 to 23 residues) and [3H]-Ac-CoA addition and measured after 60 mins by radioactive acetylation assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Saccharomyces cerevisiae |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Histone acetyltransferase GCN5 (CHEMBL4669) ↗| Type | SINGLE PROTEIN |
| Organism | Saccharomyces cerevisiae S288c |
Publication
Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.75 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1365300 | — | — | 1 | 5.54 |
| CHEMBL4168633 | — | — | 1 | 5.17 |
| CHEMBL4172975 | — | — | 1 | 5.07 |
| CHEMBL4171987 | — | — | 1 | 4.80 |
| CHEMBL4160712 | — | — | 1 | 4.72 |
| CHEMBL4159754 | — | — | 1 | 4.70 |
| CHEMBL4175431 | — | — | 1 | 4.51 |
| CHEMBL4162185 | — | — | 1 | 4.47 |
| CHEMBL4165080 | — | — | 1 | 4.46 |
| CHEMBL4170095 | — | — | 1 | 4.09 |
| CHEMBL4167662 | — | — | 1 | - |
| CHEMBL4175827 | — | — | 1 | - |
| CHEMBL4165213 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1365300 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4168633 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4172975 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4171987 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4160712 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4159754 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4175431 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4162185 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4165080 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL4170095 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL4167662 | — | IC50 | - | — | - | |
| CHEMBL4175827 | — | IC50 | - | — | - | |
| CHEMBL4165213 | — | IC50 | - | — | - |