Assay Detail
Binding
CHEMBL5261609
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Displacement of biotinylated small-molecule ligand from recombinant His-tagged BRD4 bromodomain 2 (unknown origin) measured after 10 mins by TR-FRET assay
11
Total Activities
11
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
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.09 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4519632 | — | — | 1 | 5.85 |
| CHEMBL5286608 | — | — | 1 | 5.21 |
| CHEMBL5284261 | — | — | 1 | 5.17 |
| CHEMBL5270178 | — | — | 1 | 5.08 |
| CHEMBL5285110 | — | — | 1 | 4.91 |
| CHEMBL5268936 | — | — | 1 | 4.87 |
| CHEMBL5280605 | — | — | 1 | 4.84 |
| CHEMBL5279182 | — | — | 1 | 4.76 |
| CHEMBL5282240 | — | — | 1 | - |
| CHEMBL5289762 | — | — | 1 | - |
| CHEMBL5268484 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4519632 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5286608 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL5284261 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5270178 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5285110 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL5268936 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL5280605 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL5279182 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL5282240 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5289762 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5268484 | — | IC50 | > | 20000.0 | nM | - |