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Assay Detail

CHEMBL820390

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

Binding
In vitro inhibition of Voltage-gated sodium channel by the displacement of [3H]batrachotoxin A 20-alpha-benzoate in rat brain cerebral cortex synaptoneurosomes
25
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
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

Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.
Brown ML, Zha CC, Van Dyke CC, Brown GB, Brouillette WJ.
J Med Chem (1999) 42 : 1537 -1545
PubMed 10229624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.65 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417155 1 5.30
CHEMBL39043 1 5.30
CHEMBL287713 1 5.05
CHEMBL289499 1 4.89
CHEMBL288505 1 4.41
CHEMBL16 PHENYTOIN 4.0 1 4.40
CHEMBL39889 1 4.24
CHEMBL39326 1 4.24
CHEMBL39247 1 4.02
CHEMBL290090 1 -
CHEMBL39126 2 -
CHEMBL39810 1 -
CHEMBL39377 1 -
CHEMBL108 CARBAMAZEPINE 4.0 1 -
CHEMBL38760 2 -
CHEMBL289046 1 -
CHEMBL288861 1 -
CHEMBL289431 1 -
CHEMBL290743 1 -
CHEMBL38588 1 -
CHEMBL39010 1 -
CHEMBL38675 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39043 IC50 = 5000.0 nM 5.30
CHEMBL417155 IC50 = 5000.0 nM 5.30
CHEMBL287713 IC50 = 9000.0 nM 5.05
CHEMBL289499 IC50 = 13000.0 nM 4.89
CHEMBL288505 IC50 = 39000.0 nM 4.41
CHEMBL16 PHENYTOIN IC50 = 40000.0 nM 4.40
CHEMBL39889 IC50 = 58000.0 nM 4.24
CHEMBL39326 IC50 = 58000.0 nM 4.24
CHEMBL39247 IC50 = 95000.0 nM 4.02
CHEMBL290090 IC50 = 251000.0 nM -
CHEMBL39126 IC50 = 427000.0 nM -
CHEMBL39810 IC50 = 285000.0 nM -
CHEMBL39377 IC50 = 251000.0 nM -
CHEMBL108 CARBAMAZEPINE IC50 = 131000.0 nM -
CHEMBL38760 IC50 = 225000.0 nM -
CHEMBL39126 IC50 = 427000.0 nM -
CHEMBL289046 IC50 = 851000.0 nM -
CHEMBL288861 IC50 = 162000.0 nM -
CHEMBL38675 IC50 = 700000.0 nM -
CHEMBL289431 IC50 = 2112000.0 nM -
CHEMBL290743 IC50 = 250000.0 nM -
CHEMBL38760 IC50 = 225000.0 nM -
CHEMBL38588 IC50 = 720000.0 nM -
CHEMBL39010 IC50 = 103000.0 nM -
CHEMBL38675 IC50 = 700000.0 nM -