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Assay Detail

CHEMBL4046486

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

Binding
Inhibition of Nav1.7 in adult mouse DRG neurons assessed as inhibition of fast-inactivating TTX-sensitive sodium currents
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL3414411)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C.
Bioorg Med Chem (2017) 25 : 5490 -5505
PubMed 28818462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.47 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072883 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072883 IC50 = 34.0 nM 7.47