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Assay Detail

CHEMBL4373256

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

Binding
Inhibition of Nav1.7 in mouse DRG neurons at -70 mV holding potential by patch clamp electrophysiology method
7
Total Activities
7
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 Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.
Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.
J Med Chem (2019) 62 : 831 -856
PubMed 30576602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.04 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061793 1 8.74
CHEMBL4290933 1 8.30
CHEMBL4279180 1 7.96
CHEMBL4276864 1 7.92
CHEMBL4280298 1 7.92
CHEMBL4550045 1 7.85
CHEMBL4287506 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061793 IC50 = 1.8 nM 8.74
CHEMBL4290933 IC50 = 5.0 nM 8.30
CHEMBL4279180 IC50 = 11.0 nM 7.96
CHEMBL4276864 IC50 = 12.0 nM 7.92
CHEMBL4280298 IC50 = 12.0 nM 7.92
CHEMBL4550045 IC50 = 14.0 nM 7.85
CHEMBL4287506 IC50 = 24.0 nM 7.62