Assay Detail
Binding
CHEMBL5529424
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Binding affinity to BRD4 BD2 (unknown origin) by ITC analysis
3
Total Activities
3
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
Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 7.47 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.52 |
| CHEMBL1957266 | — | — | 1 | 7.02 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL1957266 | — | Kd | = | 96.1 | nM | 7.02 |
| CHEMBL2393130 | APABETALONE | Kd | = | 135.0 | nM | 6.87 |