Assay Detail
Binding
CHEMBL4405934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to recombinant BRD3 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 | 6.10 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.16 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.69 |
| CHEMBL4549898 | — | — | 1 | 5.76 |
| CHEMBL4517875 | — | — | 1 | 5.71 |
| CHEMBL4455209 | — | — | 1 | 5.68 |
| CHEMBL4557050 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | Kd | = | 69.0 | nM | 7.16 |
| CHEMBL2393130 | APABETALONE | Kd | = | 203.0 | nM | 6.69 |
| CHEMBL4549898 | — | Kd | = | 1719.0 | nM | 5.76 |
| CHEMBL4517875 | — | Kd | = | 1962.0 | nM | 5.71 |
| CHEMBL4455209 | — | Kd | = | 2081.0 | nM | 5.68 |
| CHEMBL4557050 | — | Kd | = | 2495.0 | nM | 5.60 |