Assay Detail
Functional
CHEMBL679882
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
6
Total Activities
6
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
Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.65 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.33 |
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | 4.0 | 1 | 9.14 |
| CHEMBL1627354 | — | — | 1 | 8.46 |
| CHEMBL1627351 | — | — | 1 | 6.50 |
| CHEMBL1628199 | — | — | 1 | 6.29 |
| CHEMBL33899 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL1627354 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1627351 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL1628199 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL33899 | — | IC50 | = | 654.0 | nM | 6.18 |