Assay Detail
Functional
CHEMBL832277
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state
21
Total Activities
21
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 | 21 | 6.37 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 9.04 |
| CHEMBL12713 | SERTINDOLE | 4.0 | 1 | 7.85 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 7.74 |
| CHEMBL61301 | TECASTEMIZOLE | 2.0 | 1 | 7.55 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.55 |
| CHEMBL1108 | DROPERIDOL | 4.0 | 1 | 7.49 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.84 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 6.79 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 6.79 |
| CHEMBL1107 | HALOFANTRINE | 4.0 | 1 | 6.70 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 6.26 |
| CHEMBL537847 | — | — | 1 | 6.25 |
| CHEMBL45816 | MIBEFRADIL | 4.0 | 1 | 5.84 |
| CHEMBL2368925 | DOLASETRON | 4.0 | 1 | 5.22 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 5.00 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 4.76 |
| CHEMBL914 | FEXOFENADINE | 4.0 | 1 | 4.67 |
| CHEMBL850 | SPARFLOXACIN | 4.0 | 1 | 4.58 |
| CHEMBL583 | GREPAFLOXACIN | 4.0 | 1 | 4.11 |
| CHEMBL31 | GATIFLOXACIN | 4.0 | 1 | - |
| CHEMBL32 | MOXIFLOXACIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 0.912 | nM | 9.04 |
| CHEMBL12713 | SERTINDOLE | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL1423 | PIMOZIDE | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL61301 | TECASTEMIZOLE | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL1108 | DROPERIDOL | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 162.18 | nM | 6.79 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 162.18 | nM | 6.79 |
| CHEMBL1107 | HALOFANTRINE | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL1008 | BEPRIDIL | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL537847 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL45816 | MIBEFRADIL | IC50 | = | 1445.44 | nM | 5.84 |
| CHEMBL2368925 | DOLASETRON | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL914 | FEXOFENADINE | IC50 | = | 21379.62 | nM | 4.67 |
| CHEMBL850 | SPARFLOXACIN | IC50 | = | 26302.68 | nM | 4.58 |
| CHEMBL583 | GREPAFLOXACIN | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL31 | GATIFLOXACIN | IC50 | = | 128824.96 | nM | - |
| CHEMBL32 | MOXIFLOXACIN | IC50 | = | 117489.76 | nM | - |