Assay Detail
Binding
CHEMBL854890
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-dofetilide from hERG-expressing HEK membrane homogenates
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.72 | 5.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216104 | — | — | 1 | 5.86 |
| CHEMBL274168 | — | — | 1 | 5.60 |
| CHEMBL216554 | — | — | 1 | 5.28 |
| CHEMBL217233 | — | — | 1 | 5.24 |
| CHEMBL216180 | — | — | 1 | 5.22 |
| CHEMBL384043 | — | — | 1 | 4.70 |
| CHEMBL217435 | — | — | 1 | 4.60 |
| CHEMBL215457 | — | — | 1 | 4.57 |
| CHEMBL216524 | — | — | 1 | 4.46 |
| CHEMBL266725 | — | — | 1 | 4.32 |
| CHEMBL216680 | — | — | 1 | 4.32 |
| CHEMBL386281 | — | — | 1 | 4.29 |
| CHEMBL269352 | — | — | 1 | 4.22 |
| CHEMBL216323 | — | — | 1 | 4.07 |
| CHEMBL216482 | — | — | 1 | 4.07 |
| CHEMBL214021 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216104 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL274168 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL216554 | — | IC50 | = | 5280.0 | nM | 5.28 |
| CHEMBL217233 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL216180 | — | IC50 | = | 6080.0 | nM | 5.22 |
| CHEMBL384043 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL217435 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL215457 | — | IC50 | = | 26700.0 | nM | 4.57 |
| CHEMBL216524 | — | IC50 | = | 34600.0 | nM | 4.46 |
| CHEMBL266725 | — | IC50 | = | 47400.0 | nM | 4.32 |
| CHEMBL216680 | — | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL386281 | — | IC50 | = | 51100.0 | nM | 4.29 |
| CHEMBL269352 | — | IC50 | = | 60700.0 | nM | 4.22 |
| CHEMBL216323 | — | IC50 | = | 85200.0 | nM | 4.07 |
| CHEMBL216482 | — | IC50 | = | 85500.0 | nM | 4.07 |
| CHEMBL214021 | — | IC50 | = | 15100.0 | nM | - |