Assay Detail
Binding
CHEMBL4256580
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]GX-545 from recombinant human NaV1.7 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit after 18 hrs by liquid scintillation counting method
23
Total Activities
23
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
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.04 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290579 | — | — | 1 | 8.00 |
| CHEMBL4286076 | — | — | 1 | 8.00 |
| CHEMBL4282302 | — | — | 1 | 8.00 |
| CHEMBL4279238 | — | — | 1 | 8.00 |
| CHEMBL4285790 | — | — | 1 | 7.70 |
| CHEMBL4287156 | — | — | 1 | 7.70 |
| CHEMBL4293669 | — | — | 1 | 7.52 |
| CHEMBL4277472 | — | — | 1 | 7.52 |
| CHEMBL4293982 | — | — | 1 | 7.30 |
| CHEMBL4289803 | — | — | 1 | 7.22 |
| CHEMBL3341985 | — | — | 1 | 7.16 |
| CHEMBL4292896 | — | — | 1 | 6.96 |
| CHEMBL4282700 | — | — | 1 | 6.92 |
| CHEMBL4278206 | — | — | 1 | 6.85 |
| CHEMBL3893022 | — | — | 1 | 6.82 |
| CHEMBL4281994 | — | — | 1 | 6.80 |
| CHEMBL4281670 | — | — | 1 | 6.80 |
| CHEMBL4286121 | — | — | 1 | 6.77 |
| CHEMBL4285100 | — | — | 1 | 6.70 |
| CHEMBL4292933 | — | — | 1 | 6.02 |
| CHEMBL4289504 | — | — | 1 | 5.93 |
| CHEMBL3922136 | — | — | 1 | 5.90 |
| CHEMBL4289552 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290579 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4286076 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4282302 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4279238 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4285790 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4287156 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4293669 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4277472 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4293982 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4289803 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3341985 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4292896 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4282700 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4278206 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3893022 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4281994 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4281670 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4286121 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4285100 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4292933 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4289504 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL3922136 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4289552 | — | IC50 | = | 3880.0 | nM | 5.41 |