Assay Detail
Binding
CHEMBL805351
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Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells
15
Total Activities
15
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 | Expert |
Target
Sodium channel protein type 4 subunit alpha (CHEMBL2072) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.10 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38401 | — | — | 1 | 7.60 |
| CHEMBL37316 | — | — | 1 | 7.51 |
| CHEMBL289425 | — | — | 1 | 7.51 |
| CHEMBL37263 | — | — | 1 | 7.46 |
| CHEMBL38488 | — | — | 1 | 6.82 |
| CHEMBL287833 | — | — | 1 | 6.75 |
| CHEMBL38031 | — | — | 1 | 6.70 |
| CHEMBL41864 | — | — | 1 | 6.62 |
| CHEMBL289421 | — | — | 1 | 6.47 |
| CHEMBL38970 | — | — | 1 | 6.16 |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | 4.77 |
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | 4.62 |
| CHEMBL108 | CARBAMAZEPINE | 4.0 | 1 | 4.28 |
| CHEMBL38876 | — | — | 1 | 4.21 |
| CHEMBL39210 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38401 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL37316 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL289425 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL37263 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL38488 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL287833 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL38031 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL41864 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL289421 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL38970 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL741 | LAMOTRIGINE | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL16 | PHENYTOIN | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL108 | CARBAMAZEPINE | Ki | = | 52000.0 | nM | 4.28 |
| CHEMBL38876 | — | Ki | = | 61000.0 | nM | 4.21 |
| CHEMBL39210 | — | Ki | = | 81000.0 | nM | 4.09 |