Assay Detail
Functional
CHEMBL818551
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Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Heart |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.62 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL282841 | — | — | 1 | 7.22 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 6.92 |
| CHEMBL281072 | — | — | 1 | 6.66 |
| CHEMBL430716 | — | — | 1 | 6.52 |
| CHEMBL283710 | — | — | 1 | 5.80 |
| CHEMBL28853 | — | — | 1 | 5.79 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.60 |
| CHEMBL744 | RILUZOLE | 4.0 | 1 | 5.40 |
| CHEMBL29187 | — | — | 1 | 5.39 |
| CHEMBL282833 | — | — | 1 | 5.30 |
| CHEMBL28854 | SIPATRIGINE | 2.0 | 1 | 5.28 |
| CHEMBL29404 | ENECADIN | 2.0 | 1 | 5.11 |
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | 4.68 |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | 4.68 |
| CHEMBL79 | LIDOCAINE | 4.0 | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL282841 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL281072 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL430716 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL283710 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL28853 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL744 | RILUZOLE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL29187 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL282833 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL28854 | SIPATRIGINE | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL29404 | ENECADIN | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL16 | PHENYTOIN | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL741 | LAMOTRIGINE | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL79 | LIDOCAINE | IC50 | = | 97000.0 | nM | 4.01 |