Assay Detail
Binding
CHEMBL4013740
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Downregulation of human ERalpha in human MCF-7 cells after 24 hrs by in-cell Western immunoassay method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.39 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.52 |
| CHEMBL4078577 | — | — | 1 | 9.28 |
| CHEMBL4065838 | — | — | 1 | 8.68 |
| CHEMBL4070669 | — | — | 1 | 8.54 |
| CHEMBL4102857 | — | — | 1 | 8.37 |
| CHEMBL4099302 | — | — | 1 | 8.27 |
| CHEMBL4060067 | — | — | 1 | 8.25 |
| CHEMBL4098470 | — | — | 1 | 8.04 |
| CHEMBL4073395 | — | — | 1 | 8.00 |
| CHEMBL4100247 | — | — | 1 | 8.00 |
| CHEMBL4062045 | — | — | 1 | 7.92 |
| CHEMBL4083658 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4078577 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4065838 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4070669 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4102857 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4099302 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4060067 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4098470 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4073395 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4100247 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4062045 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4083658 | — | IC50 | = | 17.0 | nM | 7.77 |