Assay Detail
Binding
CHEMBL4710397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD2 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay
4
Total Activities
4
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
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.80 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 8.17 |
| CHEMBL4752543 | — | — | 1 | 7.75 |
| CHEMBL4743540 | — | — | 1 | 7.66 |
| CHEMBL4798353 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4752543 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4743540 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4798353 | — | IC50 | = | 25.0 | nM | 7.60 |