Assay Detail
Toxicity
CHEMBL5163410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG potassium channel expressed in CHO cells by patch-clamp assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 25 | 4.93 | 5.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5190953 | — | — | 1 | 5.21 |
| CHEMBL5207893 | — | — | 1 | 5.13 |
| CHEMBL5173113 | — | — | 1 | 4.94 |
| CHEMBL5198894 | — | — | 1 | 4.81 |
| CHEMBL5184413 | — | — | 1 | 4.56 |
| CHEMBL5198039 | — | — | 1 | - |
| CHEMBL5180046 | — | — | 1 | - |
| CHEMBL5208566 | — | — | 1 | - |
| CHEMBL5170271 | — | — | 1 | - |
| CHEMBL5202599 | — | — | 1 | - |
| CHEMBL5191391 | — | — | 1 | - |
| CHEMBL5208192 | — | — | 1 | - |
| CHEMBL5181826 | — | — | 1 | - |
| CHEMBL5198626 | — | — | 1 | - |
| CHEMBL5181850 | — | — | 1 | - |
| CHEMBL5203346 | — | — | 1 | - |
| CHEMBL5205357 | — | — | 1 | - |
| CHEMBL5171948 | — | — | 1 | - |
| CHEMBL5169445 | — | — | 1 | - |
| CHEMBL5205546 | — | — | 1 | - |
| CHEMBL5191700 | — | — | 1 | - |
| CHEMBL5171955 | — | — | 1 | - |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | - |
| CHEMBL5191161 | — | — | 1 | - |
| CHEMBL5205039 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5190953 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5207893 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5173113 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL5198894 | — | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL5184413 | — | IC50 | = | 27500.0 | nM | 4.56 |
| CHEMBL5198039 | — | IC50 | - | — | - | |
| CHEMBL5180046 | — | IC50 | - | — | - | |
| CHEMBL5208566 | — | IC50 | - | — | - | |
| CHEMBL5170271 | — | IC50 | - | — | - | |
| CHEMBL5202599 | — | IC50 | - | — | - | |
| CHEMBL5191391 | — | IC50 | - | — | - | |
| CHEMBL5208192 | — | IC50 | - | — | - | |
| CHEMBL5181826 | — | IC50 | - | — | - | |
| CHEMBL5198626 | — | IC50 | - | — | - | |
| CHEMBL5181850 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5203346 | — | IC50 | - | — | - | |
| CHEMBL5205357 | — | IC50 | - | — | - | |
| CHEMBL5171948 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5169445 | — | IC50 | - | — | - | |
| CHEMBL5205546 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5191700 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5171955 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1358 | FULVESTRANT | IC50 | - | — | - | |
| CHEMBL5191161 | — | IC50 | - | — | - | |
| CHEMBL5205039 | — | IC50 | - | — | - |