Assay Detail
Binding
CHEMBL5529426
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Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay
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 |
|---|---|---|---|
| IC50 | 3 | 6.54 | 7.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4636881 | GSK046 | — | 1 | 7.31 |
| CHEMBL4635134 | GSK620 | — | 1 | 7.09 |
| CHEMBL4639128 | GSK778 | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4636881 | GSK046 | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4635134 | GSK620 | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4639128 | GSK778 | IC50 | = | 5843.0 | nM | 5.23 |