Assay Detail
Binding
CHEMBL5131291
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.4 expressed in HEK293 cells by whole cell patch clamp electrophysiology recording
22
Total Activities
22
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 4 subunit alpha (CHEMBL2072) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Selective Inhibitors of Na<sub>V</sub>1.7 Templated on Saxitoxin as Therapeutics for Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.29 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL501134 | SAXITOXIN | — | 1 | 8.72 |
| CHEMBL5192731 | — | — | 1 | 8.70 |
| CHEMBL5189924 | — | — | 1 | 8.70 |
| CHEMBL5184022 | — | — | 1 | 7.82 |
| CHEMBL5205795 | — | — | 1 | 7.50 |
| CHEMBL5192925 | — | — | 1 | 7.48 |
| CHEMBL5204844 | — | — | 1 | 7.29 |
| CHEMBL5204544 | — | — | 1 | 7.12 |
| CHEMBL5208387 | — | — | 1 | 6.92 |
| CHEMBL5181418 | — | — | 1 | 6.52 |
| CHEMBL5196634 | — | — | 1 | 4.62 |
| CHEMBL5169661 | — | — | 1 | 4.60 |
| CHEMBL5198438 | — | — | 1 | 4.57 |
| CHEMBL5202052 | — | — | 1 | 4.18 |
| CHEMBL5197755 | — | — | 1 | 4.10 |
| CHEMBL5176104 | — | — | 1 | 4.07 |
| CHEMBL5175322 | — | — | 1 | 4.00 |
| CHEMBL5208767 | — | — | 1 | - |
| CHEMBL5192207 | — | — | 1 | - |
| CHEMBL5195962 | — | — | 1 | - |
| CHEMBL4286792 | — | — | 1 | - |
| CHEMBL5176583 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL501134 | SAXITOXIN | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5192731 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5189924 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5184022 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5205795 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5192925 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5204844 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5204544 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5208387 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5181418 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5196634 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL5169661 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5198438 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL5202052 | — | IC50 | = | 66000.0 | nM | 4.18 |
| CHEMBL5197755 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL5176104 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL5175322 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL5208767 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5192207 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5195962 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4286792 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5176583 | — | IC50 | > | 100000.0 | nM | - |