Assay Detail
Toxicity
CHEMBL5239937
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Inhibition of human ERG expressed in CHO-K1 cells by Q-patch clamp assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and <i>In Vivo</i> Efficacy in a <i>Plasmodium berghei</i> Mouse Malaria Infection Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.39 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.38 |
| CHEMBL5273046 | — | — | 1 | 7.00 |
| CHEMBL5291291 | — | — | 1 | 6.89 |
| CHEMBL5275583 | — | — | 1 | 6.60 |
| CHEMBL5280818 | — | — | 1 | 6.46 |
| CHEMBL5283963 | — | — | 1 | 6.33 |
| CHEMBL5275108 | — | — | 1 | 6.31 |
| CHEMBL5273140 | — | — | 1 | 6.20 |
| CHEMBL5267563 | — | — | 1 | 6.07 |
| CHEMBL5285111 | — | — | 1 | 6.05 |
| CHEMBL5286751 | — | — | 1 | 5.87 |
| CHEMBL5273748 | — | — | 1 | 4.54 |
| CHEMBL5291089 | — | — | 1 | - |
| CHEMBL5286661 | — | — | 1 | - |
| CHEMBL5267185 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5273046 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5291291 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5275583 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5280818 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5283963 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5275108 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5273140 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5267563 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5285111 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5286751 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL5273748 | — | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL5291089 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5286661 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5267185 | — | IC50 | > | 30000.0 | nM | - |