Assay Detail
Binding
CHEMBL5163411
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Antagonist activity at ERbeta expressed in HEK293/Gal4 cells incubated for 24 hrs in presence of di-arylpropionitrile by luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Thieno[2,3-<i>e</i>]indazole Derivatives as Novel Oral Selective Estrogen Receptor Degraders with Highly Improved Antitumor Effect and Favorable Druggability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.73 | 9.52 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.52 |
| CHEMBL5197035 | — | — | 1 | 8.70 |
| CHEMBL5185539 | — | — | 1 | 8.64 |
| CHEMBL4475463 | AMCENESTRANT | 3.0 | 1 | 8.07 |
| CHEMBL5181850 | — | — | 1 | - |
| CHEMBL5171948 | — | — | 1 | - |
| CHEMBL5205546 | — | — | 1 | - |
| CHEMBL5191161 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5197035 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5185539 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4475463 | AMCENESTRANT | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5181850 | — | IC50 | - | — | - | |
| CHEMBL5171948 | — | IC50 | - | — | - | |
| CHEMBL5205546 | — | IC50 | - | — | - | |
| CHEMBL5191161 | — | Activity | - | — | - |