Assay Detail
Binding
CHEMBL3636866
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Inhibition of human NaV1.5 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 5 subunit alpha (CHEMBL1980) ↗| 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 | 5.13 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3632696 | — | — | 1 | 5.96 |
| CHEMBL3632641 | — | — | 1 | 5.92 |
| CHEMBL3634331 | — | — | 1 | 5.72 |
| CHEMBL3632692 | — | — | 1 | 5.55 |
| CHEMBL3632694 | — | — | 1 | 5.52 |
| CHEMBL3632697 | — | — | 1 | 5.47 |
| CHEMBL3634327 | — | — | 1 | 5.47 |
| CHEMBL3634332 | — | — | 1 | 5.43 |
| CHEMBL3632691 | — | — | 1 | 5.36 |
| CHEMBL3634330 | — | — | 1 | 5.31 |
| CHEMBL3634326 | — | — | 1 | 5.28 |
| CHEMBL3632693 | — | — | 1 | 5.25 |
| CHEMBL3632695 | — | — | 1 | 5.21 |
| CHEMBL3634322 | — | — | 1 | 5.16 |
| CHEMBL3634337 | — | — | 1 | 5.15 |
| CHEMBL1200606 | MEXILETINE HYDROCHLORIDE | 4.0 | 1 | 5.11 |
| CHEMBL3634335 | — | — | 1 | 5.00 |
| CHEMBL3634336 | — | — | 1 | 4.89 |
| CHEMBL3632698 | — | — | 1 | 4.80 |
| CHEMBL3634323 | — | — | 1 | 4.77 |
| CHEMBL3634324 | — | — | 1 | 4.75 |
| CHEMBL3634321 | — | — | 1 | 4.70 |
| CHEMBL3634329 | — | — | 1 | 4.62 |
| CHEMBL3634328 | — | — | 1 | 4.48 |
| CHEMBL3634333 | — | — | 1 | 4.42 |
| CHEMBL3634334 | — | — | 1 | 4.11 |
| CHEMBL3634325 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3632696 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3632641 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3634331 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3632692 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3632694 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3632697 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3634327 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3634332 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3632691 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3634330 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3634326 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3632693 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3632695 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3634322 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3634337 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL1200606 | MEXILETINE HYDROCHLORIDE | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3634335 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3634336 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3632698 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3634323 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3634324 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3634321 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3634329 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3634328 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3634333 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL3634334 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL3634325 | — | IC50 | > | 33000.0 | nM | - |