Assay Detail
Binding
CHEMBL4415862
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Inhibition of recombinant human full length Nav1.2 co-expressed with human SCN1B in HEK293 cells measured after 20 mins at -45 mV holding potential by whole cell patch clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na<sub>V</sub>1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.36 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4580996 | — | — | 1 | 7.89 |
| CHEMBL4460028 | — | — | 1 | 7.51 |
| CHEMBL4466858 | — | — | 1 | 7.33 |
| CHEMBL4435054 | — | — | 1 | 7.18 |
| CHEMBL4471825 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4580996 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4460028 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4466858 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4435054 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4471825 | — | IC50 | = | 125.0 | nM | 6.90 |