Assay Detail
Binding
CHEMBL4351616
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Inhibition of biotinylated ligand binding to FLAG epitope-fused/His-tagged PCAF bromodomain (719 to 832 residues) (unknown origin) measured after 15 mins by alphalisa assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.59 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4103402 | — | — | 1 | 7.89 |
| CHEMBL4067343 | — | — | 1 | 7.72 |
| CHEMBL4088595 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4103402 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4067343 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4088595 | — | IC50 | = | 70.0 | nM | 7.16 |