Assay Detail
Binding
CHEMBL4011208
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Induction of ERalpha degradation in human MCF7 cells after 18 hrs by Western blot analysis
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.83 | 8.92 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.92 |
| CHEMBL4101697 | — | — | 1 | 8.74 |
| CHEMBL2137046 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4101697 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2137046 | — | Activity | - | — | - |