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Assay Detail

CHEMBL3419347

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

Binding
Inhibition of NaV1.7 in C57BL/6 mouse DRG neurons held at voltage yielding 20% inactivation and depolarized to -10 mV for 40 ms every 10 s by whole-cell patch clamp assay
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

Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Murray JK, Ligutti J, Liu D, Zou A, Poppe L, Li H, Andrews KL, Moyer BD, McDonough SI, Favreau P, Stöcklin R, Miranda LP.
J Med Chem (2015) 58 : 2299 -2314
PubMed 25658507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.44 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416886 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416886 IC50 = 3.6 nM 8.44