Assay Detail
Binding
CHEMBL3582788
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 8.88 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL226267 | ARZOXIFENE | 3.0 | 1 | 9.52 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.22 |
| CHEMBL44426 | PIPENDOXIFENE | 2.0 | 1 | 9.22 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 1 | 8.70 |
| CHEMBL195515 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL226267 | ARZOXIFENE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL44426 | PIPENDOXIFENE | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3581693 | BRILANESTRANT | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL195515 | — | IC50 | = | 18.0 | nM | 7.75 |