Assay Detail
Functional
CHEMBL1010834
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Antagonist activity at human ERalpha receptor expressed in HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEC-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.93 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481189 | — | — | 1 | 7.70 |
| CHEMBL520107 | — | — | 1 | 7.10 |
| CHEMBL519599 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481189 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL520107 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL519599 | — | IC50 | = | 1000.0 | nM | 6.00 |