Assay Detail
Functional
CHEMBL780605
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)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 7 | 6.45 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL543868 | — | — | 1 | 7.22 |
| CHEMBL542445 | — | — | 1 | 7.22 |
| CHEMBL544098 | — | — | 1 | 6.34 |
| CHEMBL103642 | — | — | 1 | 6.11 |
| CHEMBL545504 | — | — | 1 | 6.00 |
| CHEMBL28853 | — | — | 1 | 5.79 |
| CHEMBL556117 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL543868 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL542445 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL544098 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL103642 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL545504 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL28853 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL556117 | — | IC50 | > | 14000.0 | nM | - |