Assay Detail
Binding
CHEMBL804527
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In vitro inhibition of [3H]-BTX-B binding to sodium channels in rat brain synapto-neurosomes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Sodium channel alpha subunits; brain (Types I, II, III) (CHEMBL2095171) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.40 | 4.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16 | PHENYTOIN | 4.0 | 1 | 4.40 |
| CHEMBL305109 | — | — | 1 | - |
| CHEMBL62321 | — | — | 1 | - |
| CHEMBL70727 | — | — | 1 | - |
| CHEMBL72482 | — | — | 1 | - |
| CHEMBL62653 | — | — | 1 | - |
| CHEMBL443266 | — | — | 1 | - |
| CHEMBL41666 | — | — | 1 | - |
| CHEMBL695 | TRIMETHADIONE | 4.0 | 1 | - |
| CHEMBL108 | CARBAMAZEPINE | 4.0 | 1 | - |
| CHEMBL68312 | — | — | 1 | - |
| CHEMBL72245 | — | — | 1 | - |
| CHEMBL1169568 | — | — | 1 | - |
| CHEMBL40727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16 | PHENYTOIN | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL305109 | — | IC50 | = | 590000.0 | nM | - |
| CHEMBL62321 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL70727 | — | IC50 | = | 380000.0 | nM | - |
| CHEMBL72482 | — | IC50 | = | 640000.0 | nM | - |
| CHEMBL62653 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL443266 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL41666 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL695 | TRIMETHADIONE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL108 | CARBAMAZEPINE | IC50 | = | 131000.0 | nM | - |
| CHEMBL68312 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL72245 | — | IC50 | > | 800000.0 | nM | - |
| CHEMBL1169568 | — | IC50 | = | 160000.0 | nM | - |
| CHEMBL40727 | — | IC50 | > | 800000.0 | nM | - |