Assay Detail
Binding
CHEMBL3998973
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of ERalpha degradation in tamoxifen-sensitive human MCF7:WS8 cells after 24 hrs by CellTag 700 staining based In-cell western assay
12
Total Activities
9
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
Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 9.32 | 10.15 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081807 | — | — | 2 | 10.15 |
| CHEMBL4059888 | RINTODESTRANT | 1.0 | 2 | 9.62 |
| CHEMBL4094499 | — | — | 1 | 9.19 |
| CHEMBL4098867 | — | — | 1 | 9.15 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 2 | 9.10 |
| CHEMBL4070169 | — | — | 1 | 9.04 |
| CHEMBL4092208 | — | — | 1 | 8.96 |
| CHEMBL4073940 | — | — | 1 | - |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081807 | — | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4059888 | RINTODESTRANT | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4094499 | — | EC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4098867 | — | EC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3581693 | BRILANESTRANT | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4070169 | — | EC50 | = | 0.92 | nM | 9.04 |
| CHEMBL4092208 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3581693 | BRILANESTRANT | Activity | - | — | - | |
| CHEMBL4073940 | — | Activity | - | — | - | |
| CHEMBL4059888 | RINTODESTRANT | Activity | - | — | - | |
| CHEMBL4081807 | — | Activity | - | — | - | |
| CHEMBL1358 | FULVESTRANT | Activity | - | — | - |