Assay Detail
Binding
CHEMBL5037527
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Induction of degradation of ERalpha in human MCF7 cells at 72 hrs by Western blot analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.90 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080066 | — | — | 1 | 7.72 |
| CHEMBL5092560 | — | — | 1 | 7.48 |
| CHEMBL5082681 | — | — | 1 | 6.65 |
| CHEMBL5072101 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080066 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5092560 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5082681 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL5072101 | — | IC50 | = | 1800.0 | nM | 5.75 |