Assay Detail
Binding
CHEMBL4219280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay
8
Total Activities
4
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 Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.35 | 8.15 |
| Ki | 4 | 7.98 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228445 | — | — | 2 | 9.30 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 2 | 7.96 |
| CHEMBL1957266 | — | — | 2 | 7.83 |
| CHEMBL4228904 | — | — | 2 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228445 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4228445 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3581647 | BIRABRESIB | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL1957266 | — | Ki | = | 14.9 | nM | 7.83 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL1957266 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL4228904 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL4228904 | — | IC50 | = | 484.0 | nM | 6.32 |