Assay Detail
Binding
CHEMBL5577144
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Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay
12
Total Activities
12
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 |
|---|---|---|---|
| IC50 | 12 | 6.02 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.77 |
| CHEMBL5590267 | — | — | 1 | 7.70 |
| CHEMBL5590067 | — | — | 1 | 6.58 |
| CHEMBL5596020 | — | — | 1 | 6.19 |
| CHEMBL5590913 | — | — | 1 | 6.11 |
| CHEMBL5583993 | — | — | 1 | 5.82 |
| CHEMBL5591911 | — | — | 1 | 5.80 |
| CHEMBL5593005 | — | — | 1 | 5.44 |
| CHEMBL5590506 | — | — | 1 | 5.06 |
| CHEMBL5590578 | — | — | 1 | 5.04 |
| CHEMBL4648362 | GSK789 | — | 1 | 4.75 |
| CHEMBL5594256 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5590267 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5590067 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5596020 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5590913 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5583993 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5591911 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5593005 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL5590506 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL5590578 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4648362 | GSK789 | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL5594256 | — | IC50 | > | 10000.0 | nM | - |