Assay Detail
Binding
CHEMBL3583408
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Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method
4
Total Activities
4
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
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.56 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 8.21 |
| CHEMBL3581661 | — | — | 1 | 7.53 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 7.34 |
| CHEMBL2017291 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | Kd | = | 6.2 | nM | 8.21 |
| CHEMBL3581661 | — | Kd | = | 29.6 | nM | 7.53 |
| CHEMBL1232461 | MOLIBRESIB | Kd | = | 45.4 | nM | 7.34 |
| CHEMBL2017291 | — | Kd | = | 70.3 | nM | 7.15 |