Assay Detail
Functional
CHEMBL822598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | kidney |
| 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
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.62 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 8.36 |
| CHEMBL61301 | TECASTEMIZOLE | 2.0 | 1 | 7.55 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 6.82 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.79 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.72 |
| CHEMBL75880 | PERHEXILINE | 4.0 | 1 | 5.11 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL61301 | TECASTEMIZOLE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL708 | ZIPRASIDONE | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL75880 | PERHEXILINE | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 10000.0 | nM | 5.00 |