Assay Detail
ADMET
CHEMBL4180169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.5 expressed in HEK293 cells at -120 mV holding potential incubated over 5 mins measured at 15 secs interval by Qpatch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.05 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 6.70 |
| CHEMBL4210866 | — | — | 1 | 5.40 |
| CHEMBL4203948 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4210866 | — | IC50 | = | 4020.0 | nM | 5.40 |
| CHEMBL4203948 | — | IC50 | > | 10000.0 | nM | - |