Assay Detail
Binding
CHEMBL5055693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 1 hr in presence of veratridine and anthropleurin-C by sodium influx assay
17
Total Activities
17
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 5 subunit alpha (CHEMBL1980) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Acyl-sulfonamide Na<sub>v</sub>1.7 Inhibitors GDC-0276 and GDC-0310.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.76 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657939 | — | — | 1 | 6.96 |
| CHEMBL3657932 | — | — | 1 | 6.58 |
| CHEMBL5091342 | — | — | 1 | 6.23 |
| CHEMBL5082739 | — | — | 1 | 6.12 |
| CHEMBL3657855 | — | — | 1 | 6.06 |
| CHEMBL3657851 | — | — | 1 | 5.96 |
| CHEMBL3662226 | — | — | 1 | 5.96 |
| CHEMBL3657938 | — | — | 1 | 5.82 |
| CHEMBL5094715 | — | — | 1 | 5.82 |
| CHEMBL5079176 | — | — | 1 | 5.75 |
| CHEMBL5082131 | — | — | 1 | 5.41 |
| CHEMBL5080495 | — | — | 1 | 5.19 |
| CHEMBL5082321 | — | — | 1 | 5.16 |
| CHEMBL5071877 | — | — | 1 | 4.77 |
| CHEMBL5080891 | — | — | 1 | 4.57 |
| CHEMBL5083410 | — | — | 1 | - |
| CHEMBL5081884 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657939 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3657932 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5091342 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5082739 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3657855 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3657851 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3662226 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3657938 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5094715 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5079176 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5082131 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5080495 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5082321 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5071877 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5080891 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL5083410 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5081884 | — | IC50 | > | 30000.0 | nM | - |