Assay Detail
Binding
CHEMBL863591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Astemizole from hERG expressed in HEK293 cells at 10 uM
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 23 | - | - |
| Ki | 4 | 6.52 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 7.38 |
| CHEMBL1008 | BEPRIDIL | 4.0 | 1 | 6.35 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 6.29 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 6.06 |
| CHEMBL218836 | — | — | 1 | - |
| CHEMBL218991 | — | — | 1 | - |
| CHEMBL218915 | — | — | 1 | - |
| CHEMBL216669 | — | — | 1 | - |
| CHEMBL387251 | — | — | 1 | - |
| CHEMBL219647 | — | — | 1 | - |
| CHEMBL218929 | — | — | 1 | - |
| CHEMBL216666 | — | — | 1 | - |
| CHEMBL375571 | — | — | 1 | - |
| CHEMBL374493 | — | — | 1 | - |
| CHEMBL218992 | — | — | 1 | - |
| CHEMBL219803 | — | — | 1 | - |
| CHEMBL218790 | — | — | 1 | - |
| CHEMBL219074 | — | — | 1 | - |
| CHEMBL218410 | — | — | 1 | - |
| CHEMBL218834 | — | — | 1 | - |
| CHEMBL220407 | — | — | 1 | - |
| CHEMBL441705 | — | — | 1 | - |
| CHEMBL373860 | — | — | 1 | - |
| CHEMBL219592 | — | — | 1 | - |
| CHEMBL384427 | — | — | 1 | - |
| CHEMBL219072 | — | — | 1 | - |
| CHEMBL219128 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1423 | PIMOZIDE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1008 | BEPRIDIL | Ki | = | 444.0 | nM | 6.35 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 512.0 | nM | 6.29 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 869.0 | nM | 6.06 |
| CHEMBL218836 | — | Inhibition | = | 20.0 | % | - |
| CHEMBL218991 | — | Inhibition | - | % | - | |
| CHEMBL218915 | — | Inhibition | - | % | - | |
| CHEMBL216669 | — | Inhibition | - | % | - | |
| CHEMBL387251 | — | Inhibition | - | % | - | |
| CHEMBL219647 | — | Inhibition | - | % | - | |
| CHEMBL218929 | — | Inhibition | - | % | - | |
| CHEMBL216666 | — | Inhibition | = | 66.0 | % | - |
| CHEMBL375571 | — | Inhibition | = | 31.0 | % | - |
| CHEMBL374493 | — | Inhibition | = | 16.0 | % | - |
| CHEMBL218992 | — | Inhibition | = | 8.0 | % | - |
| CHEMBL219803 | — | Inhibition | = | 8.0 | % | - |
| CHEMBL218790 | — | Inhibition | = | 73.0 | % | - |
| CHEMBL219074 | — | Inhibition | = | 21.0 | % | - |
| CHEMBL218410 | — | Inhibition | = | 9.0 | % | - |
| CHEMBL218834 | — | Inhibition | = | 8.0 | % | - |
| CHEMBL220407 | — | Inhibition | = | 6.0 | % | - |
| CHEMBL441705 | — | Inhibition | = | 45.0 | % | - |
| CHEMBL373860 | — | Inhibition | = | 16.0 | % | - |
| CHEMBL219592 | — | Inhibition | = | 34.0 | % | - |
| CHEMBL384427 | — | Inhibition | = | 26.0 | % | - |
| CHEMBL219072 | — | Inhibition | = | 55.0 | % | - |
| CHEMBL219128 | — | Inhibition | = | 13.0 | % | - |