Assay Detail
Binding
CHEMBL889312
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Blockade of hERG expressed in HEK293 cells by whole-cell patch clamp method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.28 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 8.04 |
| CHEMBL227000 | — | — | 1 | 6.51 |
| CHEMBL227134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473 | DOFETILIDE | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL227000 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL227134 | — | IC50 | < | 3.0 | nM | - |