Assay Detail
Binding
CHEMBL5326439
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Antagonist activity against ERalpha in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.11 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 10.01 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.38 |
| CHEMBL5404063 | — | — | 1 | 7.40 |
| CHEMBL5412790 | — | — | 1 | 7.27 |
| CHEMBL5405944 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489 | AFIMOXIFENE | EC50 | = | 0.0987 | nM | 10.01 |
| CHEMBL1358 | FULVESTRANT | EC50 | = | 0.418 | nM | 9.38 |
| CHEMBL5404063 | — | EC50 | = | 39.6 | nM | 7.40 |
| CHEMBL5412790 | — | EC50 | = | 53.5 | nM | 7.27 |
| CHEMBL5405944 | — | EC50 | = | 332.0 | nM | 6.48 |