Assay Detail
Functional
CHEMBL832278
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
A two-state homology model of the hERG K+ channel: application to ligand binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.19 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 8.19 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 7.45 |
| CHEMBL17157 | TERFENADINE | 4.0 | 1 | 6.89 |
| CHEMBL708 | ZIPRASIDONE | 4.0 | 1 | 6.82 |
| CHEMBL94454 | MIZOLASTINE | 4.0 | 1 | 6.45 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 5.83 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 5.47 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 5.42 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 5.24 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 5.24 |
| CHEMBL75880 | PERHEXILINE | 4.0 | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1729 | CISAPRIDE | IC50 | = | 6.457 | nM | 8.19 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 35.48 | nM | 7.45 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 128.82 | nM | 6.89 |
| CHEMBL708 | ZIPRASIDONE | IC50 | = | 151.36 | nM | 6.82 |
| CHEMBL94454 | MIZOLASTINE | IC50 | = | 354.81 | nM | 6.45 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL289469 | GRANISETRON | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL370805 | COCAINE | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL75880 | PERHEXILINE | IC50 | = | 7762.47 | nM | 5.11 |