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Assay Detail

CHEMBL4179932

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

Binding
Inhibition of recombinant human Nav1.7 expressed in HEK293 cells by voltage clamp electrophysiology method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.
Storer RI, Pike A, Swain NA, Alexandrou AJ, Bechle BM, Blakemore DC, Brown AD, Castle NA, Corbett MS, Flanagan NJ, Fengas D, Johnson MS, Jones LH, Marron BE, Payne CE, Printzenhoff D, Rawson DJ, Rose CR, Ryckmans T, Sun J, Theile JW, Torella R, Tseng E, Warmus JS.
Bioorg Med Chem Lett (2017) 27 : 4805 -4811
PubMed 29029933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.96 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325014 PF-05089771 2.0 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325014 PF-05089771 IC50 = 11.0 nM 7.96