Assay Detail
Binding
CHEMBL4612475
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 1 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
22
Total Activities
22
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 | 22 | 6.98 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648912 | — | — | 1 | 8.23 |
| CHEMBL4640025 | — | — | 1 | 8.08 |
| CHEMBL4647718 | — | — | 1 | 8.03 |
| CHEMBL4633289 | — | — | 1 | 7.89 |
| CHEMBL4632358 | — | — | 1 | 7.89 |
| CHEMBL4644032 | — | — | 1 | 7.40 |
| CHEMBL4640133 | — | — | 1 | 7.32 |
| CHEMBL4646027 | — | — | 1 | 7.27 |
| CHEMBL4638621 | — | — | 1 | 7.08 |
| CHEMBL4637378 | — | — | 1 | 7.05 |
| CHEMBL4646327 | — | — | 1 | 7.02 |
| CHEMBL4644443 | — | — | 1 | 6.80 |
| CHEMBL4649774 | — | — | 1 | 6.79 |
| CHEMBL4632925 | — | — | 1 | 6.76 |
| CHEMBL4647786 | — | — | 1 | 6.76 |
| CHEMBL4635722 | — | — | 1 | 6.75 |
| CHEMBL1957266 | — | — | 1 | 6.70 |
| CHEMBL4639392 | — | — | 1 | 6.22 |
| CHEMBL4636280 | — | — | 1 | 6.00 |
| CHEMBL4634252 | — | — | 1 | 5.93 |
| CHEMBL4642629 | — | — | 1 | 5.85 |
| CHEMBL4644325 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648912 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4640025 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4647718 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4633289 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4632358 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL4644032 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL4640133 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4646027 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4638621 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4637378 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4646327 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4644443 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4649774 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4632925 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4647786 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4635722 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1957266 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4639392 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4636280 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4634252 | — | IC50 | = | 1181.0 | nM | 5.93 |
| CHEMBL4642629 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4644325 | — | IC50 | = | 1434.0 | nM | 5.84 |