Assay Detail
Binding
CHEMBL768686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Potassium channel HERG
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.27 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 9.05 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 8.52 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 7.75 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 7.33 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 7.25 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 6.72 |
| CHEMBL583 | GREPAFLOXACIN | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL12713 | SERTINDOLE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1423 | PIMOZIDE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1729 | CISAPRIDE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL583 | GREPAFLOXACIN | IC50 | = | 50000.0 | nM | 4.30 |