Assay Detail
Binding
CHEMBL5264188
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]GX-545 from human Nav1.7 alpha subunit expressed in HEK293 cells co-expressing beta1 subunit by liquid scintillation counting analysis
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 | 6.96 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657851 | — | — | 1 | 8.22 |
| CHEMBL3657937 | — | — | 1 | 8.10 |
| CHEMBL3662218 | — | — | 1 | 8.00 |
| CHEMBL3662190 | — | — | 1 | 7.82 |
| CHEMBL3662077 | — | — | 1 | 7.82 |
| CHEMBL3657836 | — | — | 1 | 7.82 |
| CHEMBL5272143 | — | — | 1 | 7.77 |
| CHEMBL3662236 | — | — | 1 | 7.66 |
| CHEMBL5279943 | — | — | 1 | 7.55 |
| CHEMBL3657998 | — | — | 1 | 7.48 |
| CHEMBL3657945 | — | — | 1 | 7.43 |
| CHEMBL3341985 | — | — | 1 | 7.16 |
| CHEMBL3657950 | — | — | 1 | 7.03 |
| CHEMBL3662235 | — | — | 1 | 6.75 |
| CHEMBL3657936 | — | — | 1 | 6.54 |
| CHEMBL3658006 | — | — | 1 | 6.52 |
| CHEMBL3657814 | — | — | 1 | 6.48 |
| CHEMBL3657811 | — | — | 1 | 6.45 |
| CHEMBL3657828 | — | — | 1 | 6.30 |
| CHEMBL3657895 | — | — | 1 | 6.28 |
| CHEMBL3654180 | — | — | 1 | 6.19 |
| CHEMBL3657912 | — | — | 1 | 5.92 |
| CHEMBL3657859 | — | — | 1 | 5.64 |
| CHEMBL3657964 | — | — | 1 | 5.62 |
| CHEMBL3657810 | — | — | 1 | 5.57 |
| CHEMBL3657822 | — | — | 1 | - |
| CHEMBL5270997 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657851 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3657937 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3662218 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3662190 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3662077 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3657836 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5272143 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3662236 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5279943 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3657998 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3657945 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3341985 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3657950 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3662235 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3657936 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3658006 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL3657814 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3657811 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL3657828 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3657895 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3654180 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL3657912 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3657859 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3657964 | — | IC50 | = | 2398.0 | nM | 5.62 |
| CHEMBL3657810 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3657822 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5270997 | — | IC50 | > | 10000.0 | nM | - |