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Assay Detail

CHEMBL4184688

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

Binding
Inhibition of human Nav1.5 channel expressed in HEK293 cells at holding potential of -70 mV by whole cell patch clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 5 subunit alpha (CHEMBL1980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K+ channel.
Vaz RJ, Kang J, Luo Y, Rampe D.
Bioorg Med Chem Lett (2018) 28 : 446 -451
PubMed 29274816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.47 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL841 LOPERAMIDE 4.0 1 6.62
CHEMBL1627 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL841 LOPERAMIDE IC50 = 239.0 nM 6.62
CHEMBL1627 IC50 = 483.0 nM 6.32