Assay Detail
Functional
CHEMBL1227817
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Antagonist activity at human wild type ERalpha expressed in HEK293T cells co-expressing ERE assessed as inhibition of estradiol-induced transactivation by luciferase reporter gene assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.31 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 9.52 |
| CHEMBL1222036 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1222036 | — | IC50 | = | 82.0 | nM | 7.09 |