Assay Detail
Binding
CHEMBL858932
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]-labeled MK499 from cloned hERG potassium channel expressed in HEK cells
12
Total Activities
12
Compounds Tested
1
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
Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.10 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202775 | — | — | 1 | 6.72 |
| CHEMBL201362 | — | — | 1 | 6.62 |
| CHEMBL202417 | — | — | 1 | 6.57 |
| CHEMBL382803 | — | — | 1 | 6.44 |
| CHEMBL382848 | — | — | 1 | 6.38 |
| CHEMBL202141 | — | — | 1 | 5.85 |
| CHEMBL319118 | — | — | 1 | 5.75 |
| CHEMBL202568 | — | — | 1 | 5.32 |
| CHEMBL379010 | — | — | 1 | 5.24 |
| CHEMBL382720 | — | — | 1 | - |
| CHEMBL383743 | — | — | 1 | - |
| CHEMBL201192 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202775 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL201362 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL202417 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL382803 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL382848 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL202141 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL319118 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL202568 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL379010 | — | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL382720 | — | Ki | > | 6000.0 | nM | - |
| CHEMBL383743 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL201192 | — | Ki | > | 6000.0 | nM | - |