Assay Detail
Binding
CHEMBL4739475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Nav1.5alpha expressed in HEK293 cells incubated for 10 mins by voltage clamp method
6
Total Activities
6
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
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.59 | 4.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4473654 | — | — | 1 | 4.66 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | — | 1 | 4.52 |
| CHEMBL945 | AMILORIDE | 4.0 | 1 | - |
| CHEMBL4513418 | — | — | 1 | - |
| CHEMBL4217043 | — | — | 1 | - |
| CHEMBL4213248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4473654 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL501701 | N,N-HEXAMETHYLENEAMILORIDE | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL945 | AMILORIDE | IC50 | > | 30000.0 | nM | - |
| CHEMBL4513418 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4217043 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4213248 | — | IC50 | < | 3000.0 | nM | - |