Assay Detail
Binding
CHEMBL1025443
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method
9
Total Activities
9
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 2 subunit alpha (CHEMBL4187) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2,4(5)-diarylimidazoles as inhibitors of hNaV1.2 sodium channels: pharmacological evaluation and structure-property relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.66 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL510722 | — | — | 1 | 6.70 |
| CHEMBL467700 | — | — | 1 | 5.85 |
| CHEMBL503978 | — | — | 1 | 5.85 |
| CHEMBL468120 | — | — | 1 | 5.60 |
| CHEMBL305200 | — | — | 1 | 5.57 |
| CHEMBL327027 | — | — | 1 | 4.39 |
| CHEMBL467919 | — | — | 1 | - |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | - |
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL510722 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL467700 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL503978 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL468120 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL305200 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL327027 | — | IC50 | = | 40600.0 | nM | 4.39 |
| CHEMBL467919 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL741 | LAMOTRIGINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL16 | PHENYTOIN | IC50 | > | 100000.0 | nM | - |