Assay Detail
Binding
CHEMBL3390669
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.7 expressed in HEK cells assessed as reduction in sodium current at -60 mV holding potential by PatchXpress platform based whole cell patch clamp electrophysiological assay
32
Total Activities
30
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
The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.46 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3325528 | — | — | 1 | 9.05 |
| CHEMBL3325526 | — | — | 1 | 8.96 |
| CHEMBL3325527 | — | — | 1 | 8.59 |
| CHEMBL3325524 | — | — | 2 | 8.48 |
| CHEMBL3325537 | — | — | 1 | 8.40 |
| CHEMBL3325523 | — | — | 1 | 8.17 |
| CHEMBL3325538 | — | — | 1 | 8.15 |
| CHEMBL3325522 | — | — | 1 | 8.10 |
| CHEMBL3325551 | — | — | 1 | 7.96 |
| CHEMBL3325536 | — | — | 2 | 7.96 |
| CHEMBL3325529 | — | — | 1 | 7.89 |
| CHEMBL3325544 | — | — | 1 | 7.64 |
| CHEMBL3325532 | — | — | 1 | 7.50 |
| CHEMBL3325548 | — | — | 1 | 7.48 |
| CHEMBL3325539 | — | — | 1 | 7.42 |
| CHEMBL3325533 | — | — | 1 | 7.30 |
| CHEMBL3325530 | — | — | 1 | 7.29 |
| CHEMBL3325549 | — | — | 1 | 7.28 |
| CHEMBL3325546 | — | — | 1 | 7.15 |
| CHEMBL3325550 | — | — | 1 | 7.12 |
| CHEMBL3325531 | — | — | 1 | 7.09 |
| CHEMBL3325542 | — | — | 1 | 7.08 |
| CHEMBL3325543 | — | — | 1 | 6.94 |
| CHEMBL3325540 | — | — | 1 | 6.89 |
| CHEMBL3325535 | — | — | 1 | 6.79 |
| CHEMBL3325547 | — | — | 1 | 6.77 |
| CHEMBL3325541 | — | — | 1 | 6.71 |
| CHEMBL3325525 | — | — | 1 | 6.62 |
| CHEMBL3325534 | — | — | 1 | 6.55 |
| CHEMBL3325545 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3325528 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3325526 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3325527 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3325524 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3325537 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3325523 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3325538 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3325522 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3325551 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3325536 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3325529 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3325544 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3325532 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3325548 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3325539 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3325533 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3325530 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3325549 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3325524 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3325546 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3325550 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3325531 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3325542 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3325543 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3325540 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3325535 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3325547 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3325541 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3325525 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL3325534 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3325536 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL3325545 | — | IC50 | = | 1889.0 | nM | 5.72 |