Assay Detail
Binding
CHEMBL677746
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 5 | 7.37 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 8.40 |
| CHEMBL44426 | PIPENDOXIFENE | 2.0 | 1 | 7.40 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 7.37 |
| CHEMBL46740 | BAZEDOXIFENE | 4.0 | 1 | 7.07 |
| CHEMBL46903 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL46740 | BAZEDOXIFENE | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL46903 | — | IC50 | = | 242.0 | nM | 6.62 |