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Assay Detail

CHEMBL752562

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

Binding
Binding of [3H]batrachotoxin (BTX) to rat brain sodium channel
4
Total Activities
4
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

Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.
Pevarello P, Traquandi G, Bonsignori A, McArthur RA, Maj R, Caccia C, Salvati P, Varasi M.
Bioorg Med Chem Lett (1999) 9 : 1783 -1788
PubMed 10406642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.46 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22207 RACEMETHORPHAN 2.0 1 5.89
CHEMBL51777 1 5.58
CHEMBL52539 1 5.28
CHEMBL48582 SAFINAMIDE MESYLATE 4.0 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22207 RACEMETHORPHAN IC50 = 1300.0 nM 5.89
CHEMBL51777 IC50 = 2600.0 nM 5.58
CHEMBL52539 IC50 = 5300.0 nM 5.28
CHEMBL48582 SAFINAMIDE MESYLATE IC50 = 8200.0 nM 5.09