Assay Detail
Binding
CHEMBL3582786
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-E2 from estrogen receptor-beta (unknown origin) by scintillation counting analysis
5
Total Activities
5
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
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.72 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195515 | — | — | 1 | 8.52 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 1 | 8.06 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 7.68 |
| CHEMBL226267 | ARZOXIFENE | 3.0 | 1 | 6.62 |
| CHEMBL44426 | PIPENDOXIFENE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195515 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3581693 | BRILANESTRANT | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL226267 | ARZOXIFENE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | - | — | - |