Assay Detail
Binding
CHEMBL4151744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal dextran-treated FBS incubated for 4 hrs by SP1 and anti-ER rabbit monocolnal antibody based in-cell Western assay
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 9.41 | 10.00 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4164869 | — | — | 1 | 10.00 |
| CHEMBL4164133 | — | — | 1 | 10.00 |
| CHEMBL4176563 | — | — | 1 | 9.70 |
| CHEMBL4171332 | — | — | 1 | 9.70 |
| CHEMBL4175085 | — | — | 1 | 9.70 |
| CHEMBL4164447 | — | — | 1 | 9.70 |
| CHEMBL4168008 | — | — | 1 | 9.70 |
| CHEMBL4174789 | — | — | 1 | 9.70 |
| CHEMBL4163562 | — | — | 1 | 9.70 |
| CHEMBL4167575 | — | — | 1 | 9.70 |
| CHEMBL4171078 | — | — | 1 | 9.70 |
| CHEMBL4163162 | — | — | 1 | 9.70 |
| CHEMBL4161695 | — | — | 1 | 9.52 |
| CHEMBL4175179 | — | — | 1 | 9.52 |
| CHEMBL4165523 | — | — | 1 | 9.52 |
| CHEMBL4160734 | — | — | 1 | 9.52 |
| CHEMBL4169918 | — | — | 1 | 9.52 |
| CHEMBL4167152 | — | — | 1 | 9.40 |
| CHEMBL4169959 | — | — | 1 | 9.40 |
| CHEMBL4162508 | — | — | 1 | 9.40 |
| CHEMBL4161455 | — | — | 1 | 9.40 |
| CHEMBL4169627 | — | — | 1 | 9.40 |
| CHEMBL4165638 | — | — | 1 | 9.30 |
| CHEMBL4175025 | — | — | 1 | 9.15 |
| CHEMBL4159755 | — | — | 1 | 9.05 |
| CHEMBL4159900 | — | — | 1 | 8.85 |
| CHEMBL4170549 | — | — | 1 | 8.82 |
| CHEMBL4173984 | — | — | 1 | 8.24 |
| CHEMBL4159656 | — | — | 1 | 8.01 |
| CHEMBL2137046 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4164869 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4164133 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4176563 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4171332 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4175085 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4164447 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4168008 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4174789 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4163562 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4167575 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4171078 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4163162 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4175179 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4161695 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4160734 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4169918 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4165523 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4167152 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4169959 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4162508 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4161455 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4169627 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4165638 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4175025 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4159755 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4159900 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4170549 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4173984 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4159656 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL2137046 | — | Activity | = | 0.1 | nM | - |
| CHEMBL68055 | ACOLBIFENE | Activity | - | — | - | |
| CHEMBL1358 | FULVESTRANT | Activity | = | 0.1 | nM | - |