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Assay Detail

CHEMBL5224985

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

Binding
Inhibition of human Nav1.5 in inactivated condition by automated patch-clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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

Inhibition of Na<sub>V</sub>1.7: the possibility of ideal analgesics.
Kitano Y, Shinozuka T.
RSC Med Chem (2022) 13 : 895 -920
PubMed 36092147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.56 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558 MEXILETINE 4.0 1 4.82
CHEMBL79 LIDOCAINE 4.0 1 4.30
CHEMBL5275826 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558 MEXILETINE IC50 = 15000.0 nM 4.82
CHEMBL79 LIDOCAINE IC50 = 50000.0 nM 4.30
CHEMBL5275826 IC50 > 100000.0 nM -