Assay Detail
Binding
CHEMBL3119943
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Modulation of human Nav1.4 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology
23
Total Activities
23
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 4 subunit alpha (CHEMBL2072) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2-aminoimidazoles as voltage-gated sodium channel modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.85 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79 | LIDOCAINE | 4.0 | 1 | 5.70 |
| CHEMBL3113255 | — | — | 1 | 4.85 |
| CHEMBL3113248 | — | — | 1 | 4.82 |
| CHEMBL3113263 | — | — | 1 | 4.60 |
| CHEMBL3113254 | — | — | 1 | 4.58 |
| CHEMBL3113251 | — | — | 1 | 4.55 |
| CHEMBL3112596 | — | — | 1 | - |
| CHEMBL3113243 | — | — | 1 | - |
| CHEMBL3113261 | — | — | 1 | - |
| CHEMBL3113260 | — | — | 1 | - |
| CHEMBL3113259 | — | — | 1 | - |
| CHEMBL3113258 | — | — | 1 | - |
| CHEMBL3113257 | — | — | 1 | - |
| CHEMBL3113256 | — | — | 1 | - |
| CHEMBL3113252 | — | — | 1 | - |
| CHEMBL3113250 | — | — | 1 | - |
| CHEMBL3113249 | — | — | 1 | - |
| CHEMBL3113247 | — | — | 1 | - |
| CHEMBL3113246 | — | — | 1 | - |
| CHEMBL3113245 | — | — | 1 | - |
| CHEMBL3113244 | — | — | 1 | - |
| CHEMBL3113262 | — | — | 1 | - |
| CHEMBL3113253 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79 | LIDOCAINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3113255 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3113248 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3113263 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3113254 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3113251 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3112596 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113243 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113261 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113260 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113259 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113258 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113257 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113256 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113252 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113250 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113249 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113247 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113246 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113245 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113244 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113262 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3113253 | — | IC50 | > | 30000.0 | nM | - |