Assay Detail
Functional
CHEMBL710408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.39 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 9.14 |
| CHEMBL44426 | PIPENDOXIFENE | 2.0 | 1 | 8.82 |
| CHEMBL46740 | BAZEDOXIFENE | 4.0 | 1 | 8.43 |
| CHEMBL46903 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL46740 | BAZEDOXIFENE | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL46903 | — | IC50 | = | 69.0 | nM | 7.16 |