Assay Detail
Binding
CHEMBL820388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]BTX-B binding to neurotoxin site 2 of sodium channel of rat cerebral cortex synaptoneurosomes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Sodium channel alpha subunits; brain (Types I, II, III) (CHEMBL2095171) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.00 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL40 | PHENOBARBITAL | 4.0 | 1 | 5.60 |
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | 4.40 |
| CHEMBL741 | LAMOTRIGINE | 4.0 | 1 | - |
| CHEMBL108 | CARBAMAZEPINE | 4.0 | 1 | - |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | - |
| CHEMBL29740 | — | — | 1 | - |
| CHEMBL340064 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL40 | PHENOBARBITAL | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL16 | PHENYTOIN | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL741 | LAMOTRIGINE | IC50 | = | 114000.0 | nM | - |
| CHEMBL108 | CARBAMAZEPINE | IC50 | = | 131000.0 | nM | - |
| CHEMBL12 | DIAZEPAM | IC50 | = | 152000.0 | nM | - |
| CHEMBL29740 | — | IC50 | = | 489000.0 | nM | - |
| CHEMBL340064 | — | IC50 | = | 170000.0 | nM | - |