Assay Detail
Binding
CHEMBL4308797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of ERalpha degradation in human MCF7 cells assessed as downregulation of ER alpha receptor expression measured after 18 to 22 hrs by immunofluorescence assay
7
Total Activities
7
Compounds Tested
1
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
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 9.06 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4528514 | — | — | 1 | 10.10 |
| CHEMBL4591926 | — | — | 1 | 9.60 |
| CHEMBL3623004 | AZD-9496 | 1.0 | 1 | 9.50 |
| CHEMBL4447306 | — | — | 1 | 8.90 |
| CHEMBL4587197 | — | — | 1 | 8.80 |
| CHEMBL4516412 | — | — | 1 | 8.70 |
| CHEMBL4452972 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4528514 | — | IC50 | = | 0.07943 | nM | 10.10 |
| CHEMBL4591926 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3623004 | AZD-9496 | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4447306 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL4587197 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4516412 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4452972 | — | IC50 | = | 15.85 | nM | 7.80 |