Assay Detail
Binding
CHEMBL4122988
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Inhibition of BRD4 (unknown origin)
5
Total Activities
5
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
Straightforward hit identification approach in fragment-based discovery of bromodomain-containing protein 4 (BRD4) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.32 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 9.00 |
| CHEMBL4303404 | PELABRESIB | 3.0 | 1 | 7.75 |
| CHEMBL4127310 | — | — | 1 | 7.00 |
| CHEMBL2179387 | — | — | 1 | 6.66 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4303404 | PELABRESIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4127310 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2179387 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 630.0 | nM | 6.20 |