Assay Detail
Binding
CHEMBL871230
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Displacement of labeled MK-499 from cloned hERG channel expressed in HEK cells
14
Total Activities
14
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
NK1 antagonists based on seven membered lactam scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.46 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380388 | — | — | 1 | 5.85 |
| CHEMBL210630 | — | — | 1 | 5.75 |
| CHEMBL209456 | — | — | 1 | 5.62 |
| CHEMBL378663 | — | — | 1 | 5.27 |
| CHEMBL209240 | — | — | 1 | 5.17 |
| CHEMBL209407 | — | — | 1 | 5.07 |
| CHEMBL380680 | — | — | 1 | - |
| CHEMBL209657 | — | — | 1 | - |
| CHEMBL210365 | — | — | 1 | - |
| CHEMBL413279 | — | — | 1 | - |
| CHEMBL425956 | — | — | 1 | - |
| CHEMBL382255 | — | — | 1 | - |
| CHEMBL437878 | — | — | 1 | - |
| CHEMBL379816 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380388 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL210630 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL209456 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL378663 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL209240 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL209407 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL380680 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL209657 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL210365 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL413279 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL425956 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL382255 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL437878 | — | Ki | > | 9000.0 | nM | - |
| CHEMBL379816 | — | Ki | > | 9000.0 | nM | - |