Assay Detail
Binding
CHEMBL5577165
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Binding affinity to BRD4 BD2 (unknown origin) assessed as dissociation constant by BROMOscan 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
Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 6.02 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5590067 | — | — | 1 | 6.60 |
| CHEMBL5590913 | — | — | 1 | 6.28 |
| CHEMBL5590578 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5590067 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL5590913 | — | Kd | = | 530.0 | nM | 6.28 |
| CHEMBL5590578 | — | Kd | = | 6500.0 | nM | 5.19 |