Assay Detail
Binding
CHEMBL818548
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Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 5.92 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29188 | LOMERIZINE | 2.0 | 1 | 7.58 |
| CHEMBL282833 | — | — | 1 | 7.34 |
| CHEMBL430716 | — | — | 1 | 6.92 |
| CHEMBL281724 | LUBELUZOLE | 2.0 | 1 | 6.55 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 1 | 6.46 |
| CHEMBL29187 | — | — | 1 | 5.96 |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | 5.77 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.60 |
| CHEMBL29835 | BESIPIRDINE | 2.0 | 1 | 5.26 |
| CHEMBL29358 | — | — | 1 | 4.60 |
| CHEMBL29134 | — | — | 1 | 4.54 |
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | 4.40 |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | - |
| CHEMBL79 | LIDOCAINE | 4.0 | 1 | - |
| CHEMBL108 | CARBAMAZEPINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29188 | LOMERIZINE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL282833 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL430716 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL281724 | LUBELUZOLE | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL29187 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL29835 | BESIPIRDINE | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL29358 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL29134 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL16 | PHENYTOIN | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL741 | LAMOTRIGINE | IC50 | = | 114000.0 | nM | - |
| CHEMBL79 | LIDOCAINE | IC50 | = | 113000.0 | nM | - |
| CHEMBL108 | CARBAMAZEPINE | IC50 | = | 131000.0 | nM | - |