Assay Detail
Binding
CHEMBL4828622
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged BRD4 BD1 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 | 7.72 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854720 | — | — | 1 | 8.00 |
| CHEMBL4858472 | — | — | 1 | 7.83 |
| CHEMBL4851953 | — | — | 1 | 7.73 |
| CHEMBL4855093 | — | — | 1 | 7.71 |
| CHEMBL4864279 | — | — | 1 | 7.60 |
| CHEMBL4848064 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854720 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4858472 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL4851953 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL4855093 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL4864279 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL4848064 | — | IC50 | = | 33.7 | nM | 7.47 |