Assay Detail
Binding
CHEMBL5135965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.8 channel stably expressed in HEK293 cells assessed as sodium current flow at holding potential of -90mV by whole-cell voltage clamp assay
6
Total Activities
6
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 | Autocuration |
Target
Sodium channel protein type 8 subunit alpha (CHEMBL5202) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-Oxopyrrolidine-3-carboxamides as Na<sub>v</sub>1.8 Inhibitors for Treating Pain Disorders, Cough Disorders, and Acute and Chronic Itch Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.55 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5182397 | — | — | 1 | 8.92 |
| CHEMBL5196342 | — | — | 1 | 8.59 |
| CHEMBL5193659 | — | — | 1 | 8.54 |
| CHEMBL5194703 | — | — | 1 | 8.47 |
| CHEMBL5183619 | — | — | 1 | 8.39 |
| CHEMBL5197040 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5182397 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5196342 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5193659 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5194703 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5183619 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5197040 | — | IC50 | = | 4.2 | nM | 8.38 |