Assay Detail
Binding
CHEMBL806328
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [14C]- guanidinium influx in Chinese hamster ovary (CHO) cells expressing rat brain sodium channel type IIA (CNaIIA-1)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium channel protein type 2 subunit alpha (CHEMBL3399) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.02 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL103284 | — | — | 1 | 6.21 |
| CHEMBL320199 | — | — | 1 | 6.10 |
| CHEMBL554684 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL103284 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL320199 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL554684 | — | IC50 | = | 1800.0 | nM | 5.75 |