Assay Detail
Binding
CHEMBL1909190
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.26 | 6.98 |
| Ki | 871 | 5.38 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 7.07 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 7.05 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 2 | 6.86 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 6.49 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 6.30 |
| CHEMBL1108 | DROPERIDOL | 4.0 | 2 | 6.12 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 2 | 6.10 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 5.89 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 5.82 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 2 | 5.74 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 2 | 5.53 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 5.47 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 2 | 5.46 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 5.46 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 5.33 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 5.32 |
| CHEMBL1630579 | MYRTECAINE | 2.0 | 2 | 5.32 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 2 | 5.29 |
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 5.17 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 5.07 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 5.06 |
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 5.00 |
| CHEMBL511 | PYRILAMINE | 4.0 | 2 | 4.99 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 2 | 4.89 |
| CHEMBL549 | CITALOPRAM | 4.0 | 2 | 4.86 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 4.86 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 4.84 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 2 | 4.78 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 4.77 |
| CHEMBL1493 | FLAVOXATE | 4.0 | 2 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305660 | EBASTINE | Ki | = | 85.8 | nM | 7.07 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 88.9 | nM | 7.05 |
| CHEMBL305660 | EBASTINE | IC50 | = | 104.8 | nM | 6.98 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | IC50 | = | 108.5 | nM | 6.96 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 139.4 | nM | 6.86 |
| CHEMBL1729 | CISAPRIDE | IC50 | = | 170.1 | nM | 6.77 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 323.7 | nM | 6.49 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 395.1 | nM | 6.40 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 496.3 | nM | 6.30 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 605.8 | nM | 6.22 |
| CHEMBL1108 | DROPERIDOL | Ki | = | 759.6 | nM | 6.12 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 792.2 | nM | 6.10 |
| CHEMBL1108 | DROPERIDOL | IC50 | = | 927.2 | nM | 6.03 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 967.0 | nM | 6.01 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 1301.0 | nM | 5.89 |
| CHEMBL728 | PROCHLORPERAZINE | Ki | = | 1514.1 | nM | 5.82 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 1588.0 | nM | 5.80 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 1815.1 | nM | 5.74 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 1848.1 | nM | 5.73 |
| CHEMBL707 | DOXAZOSIN | IC50 | = | 2215.5 | nM | 5.66 |
| CHEMBL58 | MITOXANTRONE | Ki | = | 2937.0 | nM | 5.53 |
| CHEMBL723 | CARVEDILOL | Ki | = | 3374.9 | nM | 5.47 |
| CHEMBL567 | PERPHENAZINE | Ki | = | 3454.1 | nM | 5.46 |
| CHEMBL85 | RISPERIDONE | Ki | = | 3432.8 | nM | 5.46 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 3584.9 | nM | 5.45 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 4216.0 | nM | 5.38 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 4119.3 | nM | 5.38 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 4190.1 | nM | 5.38 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 4674.6 | nM | 5.33 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 4774.3 | nM | 5.32 |
| CHEMBL1630579 | MYRTECAINE | Ki | = | 4835.7 | nM | 5.32 |
| CHEMBL422 | TRIFLUOPERAZINE | Ki | = | 5100.8 | nM | 5.29 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 5827.5 | nM | 5.24 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 5705.8 | nM | 5.24 |
| CHEMBL1630579 | MYRTECAINE | IC50 | = | 5902.4 | nM | 5.23 |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | = | 6226.0 | nM | 5.21 |
| CHEMBL809 | SERTRALINE | Ki | = | 6814.1 | nM | 5.17 |
| CHEMBL809 | SERTRALINE | IC50 | = | 8317.3 | nM | 5.08 |
| CHEMBL490 | PAROXETINE | Ki | = | 8544.5 | nM | 5.07 |
| CHEMBL42 | CLOZAPINE | Ki | = | 8660.6 | nM | 5.06 |
| CHEMBL41 | FLUOXETINE | Ki | = | 10066.0 | nM | 5.00 |
| CHEMBL511 | PYRILAMINE | Ki | = | 10337.8 | nM | 4.99 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 10571.0 | nM | 4.98 |
| CHEMBL490 | PAROXETINE | IC50 | = | 10429.3 | nM | 4.98 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 12286.4 | nM | 4.91 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 12618.2 | nM | 4.90 |
| CHEMBL55 | PENTAMIDINE | Ki | = | 12880.2 | nM | 4.89 |
| CHEMBL549 | CITALOPRAM | Ki | = | 13661.8 | nM | 4.86 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 13967.9 | nM | 4.86 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 14410.6 | nM | 4.84 |