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Assay Detail

CHEMBL3806982

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

Binding
Inhibition of full length human Nav1.3 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -50 mV by automated voltage clamp analysis
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 3 subunit alpha (CHEMBL5163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood ME, Chowdhury S, Hemeon I, Bichler P, Bogucki D, Waldbrook M, Bankar G, Sojo LE, Young C, Lin S, Shuart N, Kwan R, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP, Dehnhardt CM, Mansour TS, Oballa RM, Cohen CJ, Robinette CL.
ACS Med Chem Lett (2016) 7 : 277 -282
PubMed 26985315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.03 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617063 1 5.03
CHEMBL3341983 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617063 IC50 = 9330.0 nM 5.03
CHEMBL3341983 IC50 - -