Assay Detail
Binding
CHEMBL5147706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Nav1.2 expressed in HEK293 cells incubated for 3 mins by FRET based membrane potential 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
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na<sub>v</sub>1.7/ Nav1.8 blockers for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.06 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5196338 | — | — | 1 | 5.47 |
| CHEMBL3957193 | — | — | 1 | 5.18 |
| CHEMBL3893530 | — | — | 1 | 4.89 |
| CHEMBL5186480 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5196338 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3957193 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3893530 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL5186480 | — | IC50 | = | 20000.0 | nM | 4.70 |