Assay Detail
Binding
CHEMBL5240779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay
21
Total Activities
21
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
Design, synthesis, and biological evaluation of quinoxalinone derivatives as potent BRD4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.27 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 9.15 |
| CHEMBL1957266 | — | — | 1 | 7.64 |
| CHEMBL5289077 | — | — | 1 | 7.32 |
| CHEMBL5266305 | — | — | 1 | 7.08 |
| CHEMBL5285927 | — | — | 1 | 6.99 |
| CHEMBL5272457 | — | — | 1 | 6.47 |
| CHEMBL5290271 | — | — | 1 | 6.39 |
| CHEMBL5286474 | — | — | 1 | 6.21 |
| CHEMBL5283605 | — | — | 1 | 6.12 |
| CHEMBL5280436 | — | — | 1 | 6.11 |
| CHEMBL5291169 | — | — | 1 | 5.95 |
| CHEMBL5266847 | — | — | 1 | 5.88 |
| CHEMBL5287873 | — | — | 1 | 5.83 |
| CHEMBL5267895 | — | — | 1 | 5.81 |
| CHEMBL5290197 | — | — | 1 | 5.67 |
| CHEMBL5266283 | — | — | 1 | 5.63 |
| CHEMBL5269292 | — | — | 1 | 5.60 |
| CHEMBL5277224 | — | — | 1 | 5.58 |
| CHEMBL5270976 | — | — | 1 | 5.55 |
| CHEMBL5269534 | — | — | 1 | 5.40 |
| CHEMBL5287461 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL1957266 | — | IC50 | = | 22.9 | nM | 7.64 |
| CHEMBL5289077 | — | IC50 | = | 48.3 | nM | 7.32 |
| CHEMBL5266305 | — | IC50 | = | 82.3 | nM | 7.08 |
| CHEMBL5285927 | — | IC50 | = | 102.6 | nM | 6.99 |
| CHEMBL5272457 | — | IC50 | = | 340.8 | nM | 6.47 |
| CHEMBL5290271 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL5286474 | — | IC50 | = | 620.6 | nM | 6.21 |
| CHEMBL5283605 | — | IC50 | = | 752.9 | nM | 6.12 |
| CHEMBL5280436 | — | IC50 | = | 777.0 | nM | 6.11 |
| CHEMBL5291169 | — | IC50 | = | 1134.0 | nM | 5.95 |
| CHEMBL5266847 | — | IC50 | = | 1309.0 | nM | 5.88 |
| CHEMBL5287873 | — | IC50 | = | 1481.0 | nM | 5.83 |
| CHEMBL5267895 | — | IC50 | = | 1559.0 | nM | 5.81 |
| CHEMBL5290197 | — | IC50 | = | 2117.0 | nM | 5.67 |
| CHEMBL5266283 | — | IC50 | = | 2326.0 | nM | 5.63 |
| CHEMBL5269292 | — | IC50 | = | 2514.0 | nM | 5.60 |
| CHEMBL5277224 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL5270976 | — | IC50 | = | 2827.0 | nM | 5.55 |
| CHEMBL5269534 | — | IC50 | = | 3974.0 | nM | 5.40 |
| CHEMBL5287461 | — | IC50 | = | 4218.0 | nM | 5.38 |