Assay Detail
Binding
CHEMBL4011175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of ERalpha degradation in human MCF7 cells assessed as inhibition of insulin-mediated cell proliferation after 6 days by Hoechst 33258 dye-based assay
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 | 9.45 | 10.22 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 10.22 |
| CHEMBL4101697 | — | — | 1 | 8.68 |
| CHEMBL2137046 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL4101697 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2137046 | — | Inhibition | - | % | - |