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Assay Detail

CHEMBL4813156

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

Binding
Displacement of [3H]BNZA from Nav1.5 (unknown origin)
2
Total Activities
2
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

Identification of aryl sulfonamides as novel and potent inhibitors of Na<sub>V</sub>1.5.
Sun S, Jia Q, Zenova AY, Lin S, Hussainkhel A, Mezeyova J, Chang E, Goodchild SJ, Xie Z, Lindgren A, de Boer G, Kwan R, Khakh K, Sojo L, Bichler P, Johnson JP, Empfield JR, Cohen CJ, Dehnhardt CM, Dean R.
Bioorg Med Chem Lett (2021) 45 : 128133 -128133
PubMed 34044121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.07 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854735 1 6.43
CHEMBL4849813 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854735 Ki = 370.0 nM 6.43
CHEMBL4849813 Ki = 2020.0 nM 5.70