Assay Detail
Binding
CHEMBL5264189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit at -60 mV holding potential by whole-cell patch voltage clamp electrophysiology recording
27
Total Activities
27
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 9 subunit alpha (CHEMBL4296) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na<sub>V</sub>) 1.7 with Potent Analgesic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.62 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657851 | — | — | 1 | 9.52 |
| CHEMBL3662190 | — | — | 1 | 9.22 |
| CHEMBL3662236 | — | — | 1 | 9.15 |
| CHEMBL3662077 | — | — | 1 | 8.52 |
| CHEMBL3657937 | — | — | 1 | 8.51 |
| CHEMBL5272143 | — | — | 1 | 8.30 |
| CHEMBL3341985 | — | — | 1 | 8.22 |
| CHEMBL3662218 | — | — | 1 | 8.22 |
| CHEMBL3657945 | — | — | 1 | 8.22 |
| CHEMBL3657836 | — | — | 1 | 8.22 |
| CHEMBL3657998 | — | — | 1 | 8.10 |
| CHEMBL5279943 | — | — | 1 | 8.00 |
| CHEMBL3657936 | — | — | 1 | 7.96 |
| CHEMBL3657950 | — | — | 1 | 7.82 |
| CHEMBL3657828 | — | — | 1 | 7.77 |
| CHEMBL3657811 | — | — | 1 | 7.51 |
| CHEMBL3654180 | — | — | 1 | 7.39 |
| CHEMBL3662235 | — | — | 1 | 7.37 |
| CHEMBL3657814 | — | — | 1 | 7.23 |
| CHEMBL3657895 | — | — | 1 | 7.17 |
| CHEMBL3658006 | — | — | 1 | 7.12 |
| CHEMBL3657912 | — | — | 1 | 6.58 |
| CHEMBL3657810 | — | — | 1 | 6.36 |
| CHEMBL3657859 | — | — | 1 | 6.24 |
| CHEMBL3657964 | — | — | 1 | 6.12 |
| CHEMBL3657822 | — | — | 1 | 5.66 |
| CHEMBL5270997 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657851 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3662190 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3662236 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3662077 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3657937 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5272143 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3341985 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3662218 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657945 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657836 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657998 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5279943 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3657936 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3657950 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3657828 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3657811 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3654180 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3662235 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3657814 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3657895 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3658006 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3657912 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3657810 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3657859 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3657964 | — | IC50 | = | 752.0 | nM | 6.12 |
| CHEMBL3657822 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5270997 | — | IC50 | = | 7400.0 | nM | 5.13 |