Assay Detail
Binding
CHEMBL904964
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Displacement of [3H]estradiol from human recombinant ERalpha
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.57 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL226268 | — | — | 1 | 8.11 |
| CHEMBL226327 | — | — | 1 | 7.96 |
| CHEMBL226269 | — | — | 1 | 7.76 |
| CHEMBL226329 | — | — | 1 | 7.71 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 7.69 |
| CHEMBL226267 | ARZOXIFENE | 3.0 | 1 | 7.67 |
| CHEMBL389907 | — | — | 1 | 7.57 |
| CHEMBL389683 | — | — | 1 | 7.57 |
| CHEMBL226379 | — | — | 1 | 7.45 |
| CHEMBL449038 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL226268 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL226327 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL226269 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL226329 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL226267 | ARZOXIFENE | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL389907 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL389683 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL226379 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL449038 | — | IC50 | = | 666.0 | nM | 6.18 |