Assay Detail
Binding
CHEMBL4219281
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 2 (333 to 460 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 |
|---|---|---|---|
| Ki | 4 | 7.96 | 9.00 |
| IC50 | 4 | 7.38 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4228445 | — | — | 2 | 9.00 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 2 | 8.22 |
| CHEMBL1957266 | — | — | 2 | 7.92 |
| CHEMBL4228904 | — | — | 2 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4228445 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3581647 | BIRABRESIB | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4228445 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1957266 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL1957266 | — | IC50 | = | 42.2 | nM | 7.38 |
| CHEMBL4228904 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL4228904 | — | IC50 | = | 630.0 | nM | 6.20 |