Assay Detail
Binding
CHEMBL4321987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
16
Total Activities
15
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 7 subunit alpha (CHEMBL3585) ↗| 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 | 16 | 8.00 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217988 | — | — | 1 | 11.00 |
| CHEMBL3657855 | — | — | 1 | 9.40 |
| CHEMBL3662190 | — | — | 1 | 9.22 |
| CHEMBL3318132 | — | — | 1 | 9.10 |
| CHEMBL4588728 | — | — | 1 | 9.05 |
| CHEMBL3416886 | — | — | 1 | 8.68 |
| CHEMBL3945969 | — | — | 2 | 8.49 |
| CHEMBL4454760 | — | — | 1 | 8.00 |
| CHEMBL2325014 | PF-05089771 | 2.0 | 1 | 7.96 |
| CHEMBL4547737 | — | — | 1 | 7.72 |
| CHEMBL507974 | TETRODOTOXIN | 3.0 | 1 | 7.44 |
| CHEMBL4458532 | — | — | 1 | 7.36 |
| CHEMBL3707218 | FUNAPIDE | 2.0 | 1 | 7.27 |
| CHEMBL501134 | SAXITOXIN | — | 1 | 6.39 |
| CHEMBL3544913 | VIXOTRIGINE | 3.0 | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217988 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3657855 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3662190 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3318132 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4588728 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3416886 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3945969 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4454760 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2325014 | PF-05089771 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4547737 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL507974 | TETRODOTOXIN | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4458532 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3707218 | FUNAPIDE | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3945969 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL501134 | SAXITOXIN | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3544913 | VIXOTRIGINE | IC50 | = | 32000.0 | nM | 4.50 |