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Assay Detail

CHEMBL804530

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Binding
Inhibition of binding to sodium channel of rat cerebral cortex
11
Total Activities
11
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

Bicyclic hydantoins with a bridgehead nitrogen. Comparison of anticonvulsant activities with binding to the neuronal voltage-dependent sodium channel.
Brouillette WJ, Jestkov VP, Brown ML, Akhtar MS, DeLorey TM, Brown GB.
J Med Chem (1994) 37 : 3289 -3293
PubMed 7932556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.41 4.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288505 1 4.41
CHEMBL16 PHENYTOIN 4.0 1 4.40
CHEMBL70727 1 -
CHEMBL288861 1 -
CHEMBL39010 1 -
CHEMBL41666 1 -
CHEMBL38675 1 -
CHEMBL39126 1 -
CHEMBL695 TRIMETHADIONE 4.0 1 -
CHEMBL39810 1 -
CHEMBL1169567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288505 IC50 = 39000.0 nM 4.41
CHEMBL16 PHENYTOIN IC50 = 40000.0 nM 4.40
CHEMBL70727 IC50 = 380000.0 nM -
CHEMBL288861 IC50 = 162000.0 nM -
CHEMBL39010 IC50 = 103000.0 nM -
CHEMBL41666 IC50 = 500000.0 nM -
CHEMBL38675 IC50 = 700000.0 nM -
CHEMBL39126 IC50 = 427000.0 nM -
CHEMBL695 TRIMETHADIONE IC50 > 1000000.0 nM -
CHEMBL39810 IC50 = 285000.0 nM -
CHEMBL1169567 IC50 = 160000.0 nM -