Assay Detail
Binding
CHEMBL3584940
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay
38
Total Activities
19
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
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.31 | 7.78 |
| Ki | 19 | 6.86 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3581647 | BIRABRESIB | 2.0 | 2 | 8.22 |
| CHEMBL1957266 | — | — | 2 | 7.97 |
| CHEMBL3581661 | — | — | 2 | 7.91 |
| CHEMBL3581660 | — | — | 2 | 7.79 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 2 | 7.49 |
| CHEMBL3581662 | — | — | 2 | 7.42 |
| CHEMBL3581655 | — | — | 2 | 7.15 |
| CHEMBL2017291 | — | — | 2 | 7.13 |
| CHEMBL3581659 | — | — | 2 | 7.01 |
| CHEMBL3581656 | — | — | 2 | 7.00 |
| CHEMBL3581658 | — | — | 2 | 6.87 |
| CHEMBL3581649 | — | — | 2 | 6.71 |
| CHEMBL3581657 | — | — | 2 | 6.70 |
| CHEMBL3581650 | — | — | 2 | 6.32 |
| CHEMBL3581648 | — | — | 2 | 6.08 |
| CHEMBL3581653 | — | — | 2 | 6.06 |
| CHEMBL3581654 | — | — | 2 | 5.71 |
| CHEMBL3581651 | — | — | 2 | 5.66 |
| CHEMBL3581652 | — | — | 2 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3581647 | BIRABRESIB | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1957266 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL3581661 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL3581660 | — | Ki | = | 16.1 | nM | 7.79 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL1232461 | MOLIBRESIB | Ki | = | 32.3 | nM | 7.49 |
| CHEMBL1957266 | — | IC50 | = | 35.7 | nM | 7.45 |
| CHEMBL3581661 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL3581662 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL3581660 | — | IC50 | = | 61.9 | nM | 7.21 |
| CHEMBL3581655 | — | Ki | = | 70.1 | nM | 7.15 |
| CHEMBL2017291 | — | Ki | = | 74.8 | nM | 7.13 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 98.4 | nM | 7.01 |
| CHEMBL3581659 | — | Ki | = | 98.1 | nM | 7.01 |
| CHEMBL3581656 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3581662 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL3581658 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL3581649 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL3581657 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL3581655 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL2017291 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3581659 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL3581656 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL3581650 | — | Ki | = | 478.0 | nM | 6.32 |
| CHEMBL3581658 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL3581649 | — | IC50 | = | 579.0 | nM | 6.24 |
| CHEMBL3581657 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL3581648 | — | Ki | = | 824.0 | nM | 6.08 |
| CHEMBL3581653 | — | Ki | = | 867.0 | nM | 6.06 |
| CHEMBL3581650 | — | IC50 | = | 1817.0 | nM | 5.74 |
| CHEMBL3581654 | — | Ki | = | 1948.0 | nM | 5.71 |
| CHEMBL3581651 | — | Ki | = | 2182.0 | nM | 5.66 |
| CHEMBL3581653 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL3581648 | — | IC50 | = | 2691.0 | nM | 5.57 |
| CHEMBL3581654 | — | IC50 | = | 6175.0 | nM | 5.21 |
| CHEMBL3581652 | — | Ki | = | 8322.0 | nM | 5.08 |
| CHEMBL3581651 | — | IC50 | = | 13826.0 | nM | 4.86 |
| CHEMBL3581652 | — | IC50 | = | 73970.0 | nM | 4.13 |