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Assay Detail

CHEMBL804528

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

Binding
Inhibition of [3H]batrachotoxin binding to rat brain sodium channel
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
Pevarello P, Bonsignori A, Caccia C, Amici R, McArthur RA, Fariello RG, Salvati P, Varasi M.
Bioorg Med Chem Lett (1999) 9 : 2521 -2524
PubMed 10498200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.18 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85054 1 5.96
CHEMBL52440 DEXTROMETHORPHAN 4.0 1 5.89
CHEMBL84167 1 5.85
CHEMBL85962 1 5.11
CHEMBL48582 SAFINAMIDE MESYLATE 4.0 1 5.09
CHEMBL82327 1 5.07
CHEMBL315738 1 4.95
CHEMBL85371 1 4.88
CHEMBL83621 1 4.86
CHEMBL85899 1 4.75
CHEMBL311029 1 4.58
CHEMBL315093 1 -
CHEMBL419673 1 -
CHEMBL741 LAMOTRIGINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85054 IC50 = 1100.0 nM 5.96
CHEMBL52440 DEXTROMETHORPHAN IC50 = 1300.0 nM 5.89
CHEMBL84167 IC50 = 1400.0 nM 5.85
CHEMBL85962 IC50 = 7800.0 nM 5.11
CHEMBL48582 SAFINAMIDE MESYLATE IC50 = 8200.0 nM 5.09
CHEMBL82327 IC50 = 8500.0 nM 5.07
CHEMBL315738 IC50 = 11300.0 nM 4.95
CHEMBL85371 IC50 = 13200.0 nM 4.88
CHEMBL83621 IC50 = 13900.0 nM 4.86
CHEMBL85899 IC50 = 17900.0 nM 4.75
CHEMBL311029 IC50 = 26300.0 nM 4.58
CHEMBL315093 IC50 = 145800.0 nM -
CHEMBL419673 IC50 = 150800.0 nM -
CHEMBL741 LAMOTRIGINE IC50 = 185900.0 nM -