Assay Detail
Binding
CHEMBL3636865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NaV1.1 by IonWorks quattro automated electrophysiology assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 1 subunit alpha (CHEMBL1845) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.45 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3632641 | — | — | 1 | 6.17 |
| CHEMBL3632696 | — | — | 1 | 6.10 |
| CHEMBL3632693 | — | — | 1 | 6.04 |
| CHEMBL3634332 | — | — | 1 | 6.04 |
| CHEMBL3632691 | — | — | 1 | 5.92 |
| CHEMBL3632695 | — | — | 1 | 5.82 |
| CHEMBL3632692 | — | — | 1 | 5.75 |
| CHEMBL3634336 | — | — | 1 | 5.57 |
| CHEMBL3632694 | — | — | 1 | 5.52 |
| CHEMBL3634335 | — | — | 1 | 5.52 |
| CHEMBL3632697 | — | — | 1 | 5.51 |
| CHEMBL3634330 | — | — | 1 | 5.50 |
| CHEMBL3634329 | — | — | 1 | 5.48 |
| CHEMBL3632698 | — | — | 1 | 5.48 |
| CHEMBL3634331 | — | — | 1 | 5.37 |
| CHEMBL3634322 | — | — | 1 | 5.36 |
| CHEMBL3634337 | — | — | 1 | 5.35 |
| CHEMBL3634326 | — | — | 1 | 5.32 |
| CHEMBL3634327 | — | — | 1 | 5.27 |
| CHEMBL3634324 | — | — | 1 | 5.15 |
| CHEMBL3634333 | — | — | 1 | 5.10 |
| CHEMBL1200606 | MEXILETINE HYDROCHLORIDE | 4.0 | 1 | 4.96 |
| CHEMBL3634334 | — | — | 1 | 4.72 |
| CHEMBL3634323 | — | — | 1 | 4.68 |
| CHEMBL3634328 | — | — | 1 | 4.58 |
| CHEMBL3634325 | — | — | 1 | - |
| CHEMBL3634321 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3632641 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3632696 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3632693 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3634332 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3632691 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3632695 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3632692 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3634336 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3632694 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3634335 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3632697 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3634330 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3634329 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3632698 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3634331 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL3634322 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3634337 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3634326 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3634327 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3634324 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3634333 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL1200606 | MEXILETINE HYDROCHLORIDE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3634334 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3634323 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3634328 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3634325 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3634321 | — | IC50 | > | 33000.0 | nM | - |