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Assay Detail

CHEMBL5622385

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

Binding
Inhibition of human Nav1.5 expressed in CHO cells under inactivated state by automated patch clamp electrophysiology analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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

New aryl and acylsulfonamides as state-dependent inhibitors of Na<sub>v</sub>1.3 voltage-gated sodium channel.
Zidar N, Tomašič T, Kikelj D, Durcik M, Tytgat J, Peigneur S, Rogers M, Haworth A, Kirby RW.
Eur J Med Chem (2023) 258 : 115530 -115530
PubMed 37329714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.56 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL629 AMITRIPTYLINE 4.0 1 5.92
CHEMBL5630885 1 5.52
CHEMBL5630319 1 5.47
CHEMBL5624797 1 5.46
CHEMBL5630705 1 5.43
CHEMBL5624805 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL629 AMITRIPTYLINE IC50 = 1200.0 nM 5.92
CHEMBL5630885 IC50 = 3000.0 nM 5.52
CHEMBL5630319 IC50 = 3400.0 nM 5.47
CHEMBL5624797 IC50 = 3500.0 nM 5.46
CHEMBL5630705 IC50 = 3700.0 nM 5.43
CHEMBL5624805 IC50 > 30000.0 nM -