Assay Detail
Binding
CHEMBL4012328
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress electrophysiology assay
37
Total Activities
32
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
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.42 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3930653 | — | — | 1 | 8.52 |
| CHEMBL3949474 | — | — | 1 | 8.30 |
| CHEMBL3921690 | — | — | 1 | 8.15 |
| CHEMBL3902872 | — | — | 1 | 8.15 |
| CHEMBL3966606 | — | — | 1 | 8.14 |
| CHEMBL3915688 | — | — | 2 | 8.10 |
| CHEMBL3983367 | — | — | 1 | 8.05 |
| CHEMBL3933527 | — | — | 1 | 8.00 |
| CHEMBL3965976 | — | — | 1 | 8.00 |
| CHEMBL3956563 | — | — | 1 | 8.00 |
| CHEMBL3961163 | — | — | 1 | 7.96 |
| CHEMBL3948535 | — | — | 1 | 7.96 |
| CHEMBL4084372 | — | — | 1 | 7.92 |
| CHEMBL3941727 | — | — | 1 | 7.92 |
| CHEMBL3953660 | — | — | 1 | 7.82 |
| CHEMBL3935378 | — | — | 1 | 7.77 |
| CHEMBL3946521 | — | — | 1 | 7.77 |
| CHEMBL3921528 | — | — | 1 | 7.75 |
| CHEMBL3967168 | — | — | 1 | 7.72 |
| CHEMBL3979498 | — | — | 1 | 7.68 |
| CHEMBL3935302 | — | — | 1 | 7.66 |
| CHEMBL3949600 | — | — | 1 | 7.64 |
| CHEMBL3937744 | — | — | 1 | 7.58 |
| CHEMBL3906185 | — | — | 1 | 7.57 |
| CHEMBL4073429 | — | — | 3 | 7.57 |
| CHEMBL3903048 | — | — | 1 | 7.16 |
| CHEMBL3983724 | — | — | 1 | 6.92 |
| CHEMBL4069051 | — | — | 1 | 6.80 |
| CHEMBL3926166 | — | — | 1 | 6.68 |
| CHEMBL3947470 | — | — | 3 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3930653 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3949474 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3902872 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3921690 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3966606 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3915688 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3983367 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3933527 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3956563 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3965976 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3948535 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3961163 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4084372 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3941727 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3953660 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3935378 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3946521 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3921528 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3967168 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3979498 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3935302 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3949600 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3915688 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3937744 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3906185 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4073429 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4073429 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3903048 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3983724 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4069051 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3926166 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3947470 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3928024 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3947470 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4071624 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4073429 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3947470 | — | IC50 | = | 22000.0 | nM | 4.66 |