Assay Detail
Binding
CHEMBL954009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique
5
Total Activities
5
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 5 subunit alpha (CHEMBL1980) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.42 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL486495 | — | — | 1 | 7.00 |
| CHEMBL482676 | — | — | 1 | 5.64 |
| CHEMBL521211 | — | — | 1 | 5.34 |
| CHEMBL558 | MEXILETINE | 4.0 | 1 | 4.89 |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL486495 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL482676 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL521211 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL558 | MEXILETINE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL741 | LAMOTRIGINE | IC50 | = | 62000.0 | nM | 4.21 |