Assay Detail
Binding
CHEMBL5147704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav 1.5 expressed in HEK293 cells at -90 mV holding potential by Whole cell voltage clamp electrophysiology assay
20
Total Activities
20
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 5 subunit alpha (CHEMBL1980) ↗| 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 | 20 | 4.69 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 6.19 |
| CHEMBL5196338 | — | — | 1 | 5.80 |
| CHEMBL3947741 | — | — | 1 | 5.09 |
| CHEMBL3934019 | — | — | 1 | 4.99 |
| CHEMBL3950180 | — | — | 1 | 4.50 |
| CHEMBL5186480 | — | — | 1 | 4.48 |
| CHEMBL3893530 | — | — | 1 | 4.48 |
| CHEMBL3957193 | — | — | 1 | 4.48 |
| CHEMBL3946117 | — | — | 1 | 4.48 |
| CHEMBL3971533 | — | — | 1 | 4.48 |
| CHEMBL3965189 | — | — | 1 | 4.48 |
| CHEMBL3896057 | — | — | 1 | 4.48 |
| CHEMBL3929432 | — | — | 1 | 4.48 |
| CHEMBL3969113 | — | — | 1 | 4.48 |
| CHEMBL3939162 | — | — | 1 | 4.48 |
| CHEMBL3935365 | — | — | 1 | 4.48 |
| CHEMBL3896584 | — | — | 1 | 4.48 |
| CHEMBL3910270 | — | — | 1 | 4.48 |
| CHEMBL3970885 | — | — | 1 | 4.48 |
| CHEMBL3942849 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5196338 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3947741 | — | IC50 | = | 8080.0 | nM | 5.09 |
| CHEMBL3934019 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL3950180 | — | IC50 | = | 31300.0 | nM | 4.50 |
| CHEMBL5186480 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3893530 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3957193 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3946117 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3971533 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3965189 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3896057 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3929432 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3969113 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3939162 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3935365 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3896584 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3910270 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3970885 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3942849 | — | IC50 | = | 33000.0 | nM | 4.48 |