Assay Detail
Binding
CHEMBL3584941
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay
7
Total Activities
7
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 |
|---|---|---|---|
| Ki | 7 | 7.79 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017291 | — | — | 1 | 8.05 |
| CHEMBL3581661 | — | — | 1 | 7.96 |
| CHEMBL3581662 | — | — | 1 | 7.91 |
| CHEMBL1957266 | — | — | 1 | 7.88 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.78 |
| CHEMBL3581660 | — | — | 1 | 7.68 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 7.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017291 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3581661 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL3581662 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL1957266 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL3581647 | BIRABRESIB | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL3581660 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1232461 | MOLIBRESIB | Ki | = | 56.8 | nM | 7.25 |