Assay Detail
ADMET
CHEMBL4256591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of inactivated state of recombinant human NaV1.5 expressed in HEK293 cell membranes coexpressing Nav beta1 subunit assessed as decrease in sodium current amplitude at -60 mV holding potential by PX automated voltage clamp method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗| 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 | 3 | 6.47 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4290579 | — | — | 1 | 6.96 |
| CHEMBL4279238 | — | — | 1 | 6.58 |
| CHEMBL4285790 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4290579 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4279238 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL4285790 | — | IC50 | = | 1313.0 | nM | 5.88 |