Assay Detail
Binding
CHEMBL3804575
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Nav1.2 expressed in HEK293 cells preincubated for 40 mins followed by DiSBAC2 substrate addition measured after 90 mins by FRET assay
4
Total Activities
4
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
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.76 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 6.31 |
| CHEMBL3798363 | — | — | 1 | 5.58 |
| CHEMBL3798228 | — | — | 1 | 5.40 |
| CHEMBL3798320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3798363 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3798228 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3798320 | — | IC50 | > | 20000.0 | nM | - |