Assay Detail
Binding
CHEMBL2168484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 2 subunit alpha (CHEMBL4187) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.52 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 5.96 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 5.51 |
| CHEMBL2164389 | — | — | 1 | 5.09 |
| CHEMBL2164044 | — | — | 1 | - |
| CHEMBL2164042 | — | — | 1 | - |
| CHEMBL2164373 | — | — | 1 | - |
| CHEMBL2164371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL2164389 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2164044 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2164042 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2164373 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2164371 | — | IC50 | > | 33000.0 | nM | - |