Assay Detail
Binding
CHEMBL4828623
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged BRD4 BD2 using biotin-labelled histone H4 acetylated peptide as substrate by TR-FRET assay
6
Total Activities
6
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
Substituted 2,3-Benzodiazepines Derivatives as Bromodomain BRD4 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.91 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4851953 | — | — | 1 | 7.11 |
| CHEMBL4854720 | — | — | 1 | 6.96 |
| CHEMBL4848064 | — | — | 1 | 6.93 |
| CHEMBL4864279 | — | — | 1 | 6.87 |
| CHEMBL4858472 | — | — | 1 | 6.82 |
| CHEMBL4855093 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4851953 | — | IC50 | = | 78.4 | nM | 7.11 |
| CHEMBL4854720 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4848064 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4864279 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4858472 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4855093 | — | IC50 | = | 166.0 | nM | 6.78 |