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Assay Detail

CHEMBL755450

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [3H]BTX-B binding to Neuronal voltage-dependent sodium channel of rat cerebral cortex synaptoneurosomes
13
Total Activities
13
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

Effects of log P and phenyl ring conformation on the binding of 5-phenylhydantoins to the voltage-dependent sodium channel.
Brown ML, Brown GB, Brouillette WJ.
J Med Chem (1997) 40 : 602 -607
PubMed 9046351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.27 4.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288505 1 4.41
CHEMBL16 PHENYTOIN 4.0 1 4.40
CHEMBL39889 1 4.24
CHEMBL39247 1 4.02
CHEMBL39010 1 -
CHEMBL39377 1 -
CHEMBL289431 1 -
CHEMBL290090 1 -
CHEMBL288861 1 -
CHEMBL38760 1 -
CHEMBL289046 1 -
CHEMBL38588 1 -
CHEMBL290743 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
CHEMBL39889 IC50 = 58000.0 nM 4.24
CHEMBL39247 IC50 = 95000.0 nM 4.02
CHEMBL39010 IC50 = 103000.0 nM -
CHEMBL39377 IC50 = 251000.0 nM -
CHEMBL289431 IC50 = 2112000.0 nM -
CHEMBL290090 IC50 = 251000.0 nM -
CHEMBL288861 IC50 = 162000.0 nM -
CHEMBL38760 IC50 = 225000.0 nM -
CHEMBL289046 IC50 = 851000.0 nM -
CHEMBL38588 IC50 = 720000.0 nM -
CHEMBL290743 IC50 = 250000.0 nM -