Assay Detail
Binding
CHEMBL5577176
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Inhibition of BRD4 BD1 (unknown origin)
18
Total Activities
14
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 a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.08 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5584084 | — | — | 3 | 8.30 |
| CHEMBL5590440 | — | — | 1 | 7.70 |
| CHEMBL5591882 | — | — | 2 | 7.68 |
| CHEMBL5594175 | — | — | 2 | 7.58 |
| CHEMBL5584185 | — | — | 1 | 7.31 |
| CHEMBL1957266 | — | — | 1 | 7.07 |
| CHEMBL5593182 | — | — | 1 | 7.01 |
| CHEMBL5590067 | — | — | 1 | 6.92 |
| CHEMBL5589915 | — | — | 1 | 6.85 |
| CHEMBL5591546 | — | — | 1 | 6.82 |
| CHEMBL5590578 | — | — | 1 | 6.75 |
| CHEMBL5590838 | — | — | 1 | 6.66 |
| CHEMBL5591177 | — | — | 1 | 6.62 |
| CHEMBL5590811 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5584084 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5590440 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5584084 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5591882 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5594175 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5584185 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1957266 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5593182 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5591882 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5590067 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5594175 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5589915 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5591546 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5584084 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5590578 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5590838 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5591177 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5590811 | — | IC50 | = | 1600.0 | nM | 5.80 |