Assay Detail
Binding
CHEMBL4612477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 2 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition 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
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.52 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648912 | — | — | 1 | 8.77 |
| CHEMBL4632358 | — | — | 1 | 7.90 |
| CHEMBL4640025 | — | — | 1 | 7.67 |
| CHEMBL4633289 | — | — | 1 | 7.20 |
| CHEMBL1957266 | — | — | 1 | 6.90 |
| CHEMBL4644032 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648912 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4632358 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4640025 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL4633289 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL1957266 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4644032 | — | IC50 | = | 220.0 | nM | 6.66 |