Assay Detail
Binding
CHEMBL5044429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay
5
Total Activities
5
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, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.09 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.11 |
| CHEMBL5076336 | — | — | 1 | 6.13 |
| CHEMBL5090401 | — | — | 1 | 6.08 |
| CHEMBL5080616 | — | — | 1 | 5.90 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5076336 | — | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL5090401 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL5080616 | — | IC50 | = | 1254.0 | nM | 5.90 |
| CHEMBL2393130 | APABETALONE | IC50 | = | 5697.0 | nM | 5.24 |