Assay Detail
Binding
CHEMBL5337703
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]estradiol from human ER-alpha expressed in Sf21 cells incubated for 120 mins by scintillation counting analysis
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 9.14 | 10.15 |
| IC50 | 4 | 8.60 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | 4.0 | 2 | 10.15 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 2 | 9.70 |
| CHEMBL5413467 | — | — | 2 | 8.82 |
| CHEMBL5436409 | — | — | 2 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5413467 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5413467 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5436409 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5436409 | — | IC50 | = | 45.0 | nM | 7.35 |