Assay Detail
Binding
CHEMBL4310079
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli
5
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 3 | 6.97 | 7.05 |
| IC50 | 1 | 6.03 | 6.03 |
| Ki | 1 | 6.47 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.05 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.89 |
| CHEMBL3086883 | — | — | 1 | 6.47 |
| CHEMBL4077274 | — | — | 1 | 6.03 |
| CHEMBL3770724 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL2393130 | APABETALONE | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL3086883 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4077274 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL3770724 | — | Kd | > | 75000.0 | nM | - |