Assay Detail
Binding
CHEMBL5055692
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Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 1 hr in presence of veratridine 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 7 subunit alpha (CHEMBL3585) ↗| 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 | 7.12 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3657932 | — | — | 1 | 7.85 |
| CHEMBL5094715 | — | — | 1 | 7.80 |
| CHEMBL3662226 | — | — | 1 | 7.64 |
| CHEMBL3657851 | — | — | 1 | 7.60 |
| CHEMBL5082131 | — | — | 1 | 7.58 |
| CHEMBL5071877 | — | — | 1 | 7.51 |
| CHEMBL5080495 | — | — | 1 | 7.47 |
| CHEMBL5079176 | — | — | 1 | 7.47 |
| CHEMBL5082739 | — | — | 1 | 7.42 |
| CHEMBL5080891 | — | — | 1 | 7.38 |
| CHEMBL3657855 | — | — | 1 | 7.31 |
| CHEMBL5091342 | — | — | 1 | 7.18 |
| CHEMBL3657939 | — | — | 1 | 6.96 |
| CHEMBL5082321 | — | — | 1 | 6.92 |
| CHEMBL3657938 | — | — | 1 | 6.80 |
| CHEMBL5081884 | — | — | 1 | 5.50 |
| CHEMBL5083410 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3657932 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5094715 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3662226 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3657851 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5082131 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5071877 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5080495 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5079176 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5082739 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5080891 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3657855 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5091342 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3657939 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5082321 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3657938 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5081884 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5083410 | — | IC50 | = | 25000.0 | nM | 4.60 |