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Assay Detail

CHEMBL4009752

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

Binding
Inhibition of recombinant mouse Nav1.7 expressed in HEK293 cells assessed as reduction in peak inward current at -70 mV holding potential measured after 600 secs by manual patch clamp electrophysiology assay
3
Total Activities
3
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

Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.
Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C.
J Med Chem (2017) 60 : 2513 -2525
PubMed 28234467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.64 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078268 1 8.12
CHEMBL4064193 1 7.52
CHEMBL4092078 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078268 IC50 = 7.5 nM 8.12
CHEMBL4064193 IC50 = 30.0 nM 7.52
CHEMBL4092078 IC50 = 51.0 nM 7.29