Assay Detail
Binding
CHEMBL806327
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)
12
Total Activities
12
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 | 12 | 5.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL507974 | TETRODOTOXIN | 3.0 | 1 | 8.40 |
| CHEMBL281724 | LUBELUZOLE | 2.0 | 1 | 6.58 |
| CHEMBL544330 | — | — | 1 | 5.54 |
| CHEMBL544569 | — | — | 1 | 5.48 |
| CHEMBL542191 | — | — | 1 | 5.00 |
| CHEMBL554829 | — | — | 1 | 4.83 |
| CHEMBL553355 | — | — | 1 | 4.76 |
| CHEMBL545737 | — | — | 1 | 4.42 |
| CHEMBL543152 | — | — | 1 | 4.28 |
| CHEMBL544329 | — | — | 1 | - |
| CHEMBL537480 | — | — | 1 | - |
| CHEMBL103505 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL507974 | TETRODOTOXIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL281724 | LUBELUZOLE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL544330 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL544569 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL542191 | — | IC50 | = | 9950.0 | nM | 5.00 |
| CHEMBL554829 | — | IC50 | = | 14680.0 | nM | 4.83 |
| CHEMBL553355 | — | IC50 | = | 17550.0 | nM | 4.76 |
| CHEMBL545737 | — | IC50 | = | 38020.0 | nM | 4.42 |
| CHEMBL543152 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL544329 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL537480 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL103505 | — | IC50 | > | 25000.0 | nM | - |