Assay Detail
Binding
CHEMBL4153123
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Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay
4
Total Activities
4
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 potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.29 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.16 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.69 |
| CHEMBL4176038 | — | — | 1 | 5.66 |
| CHEMBL4159382 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2393130 | APABETALONE | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4176038 | — | IC50 | = | 2193.0 | nM | 5.66 |
| CHEMBL4159382 | — | IC50 | = | 2241.0 | nM | 5.65 |