Assay Detail
Binding
CHEMBL4045005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BRD4 bromo domain 2
3
Total Activities
3
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
Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.74 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 7.17 |
| CHEMBL4079901 | — | — | 1 | 6.65 |
| CHEMBL4064933 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393130 | APABETALONE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4079901 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL4064933 | — | IC50 | = | 401.0 | nM | 6.40 |