Assay Detail
Binding
CHEMBL4619351
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis
19
Total Activities
19
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
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.73 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447340 | — | — | 1 | 10.52 |
| CHEMBL4649161 | — | — | 1 | 10.28 |
| CHEMBL4635493 | — | — | 1 | 10.19 |
| CHEMBL4646522 | — | — | 1 | 10.08 |
| CHEMBL4644486 | — | — | 1 | 10.05 |
| CHEMBL4648503 | — | — | 1 | 10.05 |
| CHEMBL4644074 | — | — | 1 | 9.82 |
| CHEMBL4641732 | — | — | 1 | 9.77 |
| CHEMBL4640902 | — | — | 1 | 9.74 |
| CHEMBL4528514 | — | — | 1 | 9.72 |
| CHEMBL4633886 | — | — | 1 | 9.72 |
| CHEMBL4645364 | — | — | 1 | 9.68 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.49 |
| CHEMBL4644611 | — | — | 1 | 9.42 |
| CHEMBL4641773 | — | — | 1 | 9.41 |
| CHEMBL4638997 | — | — | 1 | 9.28 |
| CHEMBL4634404 | — | — | 1 | 9.26 |
| CHEMBL4640074 | — | — | 1 | 9.25 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 1 | 9.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447340 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4649161 | — | IC50 | = | 0.053 | nM | 10.28 |
| CHEMBL4635493 | — | IC50 | = | 0.065 | nM | 10.19 |
| CHEMBL4646522 | — | IC50 | = | 0.083 | nM | 10.08 |
| CHEMBL4644486 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4648503 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4644074 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4641732 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4640902 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4528514 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL4633886 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL4645364 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4644611 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4641773 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4638997 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4634404 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL4640074 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL3581693 | BRILANESTRANT | IC50 | = | 0.85 | nM | 9.07 |