Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2168237

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

Binding
Inhibition of recombinant rat NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL3312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Macsari I, Besidski Y, Csjernyik G, Nilsson LI, Sandberg L, Yngve U, Ahlin K, Bueters T, Eriksson AB, Lund PE, Venyike E, Oerther S, Hygge Blakeman K, Luo L, Arvidsson PI.
J Med Chem (2012) 55 : 6866 -6880
PubMed 22770500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.69 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164373 1 7.13
CHEMBL2164389 1 7.13
CHEMBL2164371 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164373 IC50 = 74.0 nM 7.13
CHEMBL2164389 IC50 = 74.0 nM 7.13
CHEMBL2164371 IC50 = 1600.0 nM 5.80