Assay Detail
Binding
CHEMBL5163407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of ERalpha degradation in human MCF7 cells incubated for 24 hrs by Western blot analysis
50
Total Activities
50
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 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 |
|---|---|---|---|
| EC50 | 50 | 8.76 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193428 | — | — | 1 | 9.40 |
| CHEMBL5181850 | — | — | 1 | 9.40 |
| CHEMBL5174315 | — | — | 1 | 9.15 |
| CHEMBL5207484 | — | — | 1 | 9.05 |
| CHEMBL5191161 | — | — | 1 | 9.00 |
| CHEMBL5173602 | — | — | 1 | 9.00 |
| CHEMBL5177756 | — | — | 1 | 9.00 |
| CHEMBL5173113 | — | — | 1 | 8.96 |
| CHEMBL5185539 | — | — | 1 | 8.96 |
| CHEMBL5202286 | — | — | 1 | 8.92 |
| CHEMBL5197035 | — | — | 1 | 8.92 |
| CHEMBL4475463 | AMCENESTRANT | 3.0 | 1 | 8.92 |
| CHEMBL5184413 | — | — | 1 | 8.89 |
| CHEMBL5169445 | — | — | 1 | 8.89 |
| CHEMBL5205039 | — | — | 1 | 8.89 |
| CHEMBL5171948 | — | — | 1 | 8.85 |
| CHEMBL5190953 | — | — | 1 | 8.85 |
| CHEMBL5205357 | — | — | 1 | 8.74 |
| CHEMBL5171955 | — | — | 1 | 8.70 |
| CHEMBL5189071 | — | — | 1 | 8.66 |
| CHEMBL5191391 | — | — | 1 | 8.66 |
| CHEMBL5207893 | — | — | 1 | 8.66 |
| CHEMBL5180046 | — | — | 1 | 8.66 |
| CHEMBL5198039 | — | — | 1 | 8.60 |
| CHEMBL5206306 | — | — | 1 | 8.59 |
| CHEMBL5198894 | — | — | 1 | 8.59 |
| CHEMBL5203346 | — | — | 1 | 8.52 |
| CHEMBL5181826 | — | — | 1 | 8.47 |
| CHEMBL5191700 | — | — | 1 | 8.44 |
| CHEMBL5194962 | — | — | 1 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193428 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5181850 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5174315 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5207484 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5191161 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5173602 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5177756 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5173113 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5185539 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5202286 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5197035 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4475463 | AMCENESTRANT | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5169445 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5205039 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5184413 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5171948 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5190953 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5205357 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5171955 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5189071 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5191391 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5207893 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5180046 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5198039 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5198894 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5206306 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5203346 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5181826 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5191700 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5194962 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5205546 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5208566 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5207013 | — | EC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5188343 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5208191 | — | EC50 | - | — | - | |
| CHEMBL5198988 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5196349 | — | EC50 | - | — | - | |
| CHEMBL5200219 | — | EC50 | - | — | - | |
| CHEMBL5179839 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5194464 | — | EC50 | - | — | - | |
| CHEMBL5172442 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL5178968 | — | EC50 | - | — | - | |
| CHEMBL5181707 | — | EC50 | - | — | - | |
| CHEMBL5208192 | — | EC50 | - | — | - | |
| CHEMBL5170271 | — | EC50 | - | — | - | |
| CHEMBL5202599 | — | EC50 | - | — | - | |
| CHEMBL5194330 | — | EC50 | - | — | - | |
| CHEMBL5187985 | — | EC50 | - | — | - | |
| CHEMBL5198626 | — | EC50 | - | — | - | |
| CHEMBL5187550 | — | EC50 | - | — | - |