Assay Detail
Binding
CHEMBL889314
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay
6
Total Activities
6
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 |
|---|---|---|---|
| Ki | 6 | 7.21 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.54 |
| CHEMBL473 | DOFETILIDE | 4.0 | 1 | 8.11 |
| CHEMBL536480 | — | — | 1 | 7.73 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 6.74 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 6.72 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL473 | DOFETILIDE | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL536480 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL1008 | BEPRIDIL | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL45816 | MIBEFRADIL | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL42 | CLOZAPINE | Ki | = | 4060.0 | nM | 5.39 |