Assay Detail
Binding
CHEMBL4405930
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Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr 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
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 6.71 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.21 |
| CHEMBL4549898 | — | — | 1 | 7.03 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.87 |
| CHEMBL4517875 | — | — | 1 | 6.86 |
| CHEMBL4455209 | — | — | 1 | 6.17 |
| CHEMBL4557050 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL4549898 | — | Kd | = | 93.0 | nM | 7.03 |
| CHEMBL2393130 | APABETALONE | Kd | = | 135.0 | nM | 6.87 |
| CHEMBL4517875 | — | Kd | = | 139.0 | nM | 6.86 |
| CHEMBL4455209 | — | Kd | = | 684.0 | nM | 6.17 |
| CHEMBL4557050 | — | Kd | = | 718.0 | nM | 6.14 |