Assay Detail
Binding
CHEMBL4003550
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Displacement of biotinylated small molecule ligand from His/FLAG-tagged PCAF bromodomain (719 to 832 residues) (unknown origin) after 15 mins by AlphaLisa method
7
Total Activities
7
Compounds Tested
2
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 a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.92 | 7.89 |
| Kd | 2 | 5.17 | 5.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4103402 | — | — | 1 | 7.89 |
| CHEMBL4067343 | — | — | 1 | 7.72 |
| CHEMBL4088595 | — | — | 1 | 7.16 |
| CHEMBL4070058 | — | — | 1 | 6.05 |
| CHEMBL609728 | — | — | 1 | 5.80 |
| CHEMBL3775323 | — | — | 1 | 5.17 |
| CHEMBL1417210 | — | — | 1 | - |
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 |
| CHEMBL4070058 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL609728 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3775323 | — | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL1417210 | — | Kd | = | 250000.0 | nM | - |