Assay Detail
Binding
CHEMBL4321997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
7
Total Activities
7
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 10 subunit alpha (CHEMBL5451) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na<sub>V</sub>1.7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.86 | 5.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3707218 | FUNAPIDE | 2.0 | 1 | 5.32 |
| CHEMBL3544913 | VIXOTRIGINE | 3.0 | 1 | 5.22 |
| CHEMBL4217988 | — | — | 1 | 4.58 |
| CHEMBL4588728 | — | — | 1 | 4.30 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | - |
| CHEMBL507974 | TETRODOTOXIN | 3.0 | 1 | - |
| CHEMBL501134 | SAXITOXIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3707218 | FUNAPIDE | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3544913 | VIXOTRIGINE | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4217988 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4588728 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL2325014 | PF-05089771 | IC50 | > | 10000.0 | nM | - |
| CHEMBL507974 | TETRODOTOXIN | IC50 | > | 30000.0 | nM | - |
| CHEMBL501134 | SAXITOXIN | IC50 | > | 10000.0 | nM | - |