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Assay Detail

CHEMBL3636870

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

Binding
Inhibition of mouse NaV1.1 by IonWorks quattro automated electrophysiology assay
6
Total Activities
6
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 1 subunit alpha (CHEMBL4523103)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Suzuki S, Kuroda T, Kimoto H, Domon Y, Kubota K, Kitano Y, Yokoyama T, Shimizugawa A, Sugita R, Koishi R, Asano D, Tamaki K, Shinozuka T, Kobayashi H.
Bioorg Med Chem Lett (2015) 25 : 5419 -5423
PubMed 26358159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.44 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3632695 1 6.17
CHEMBL3634332 1 6.16
CHEMBL3632698 1 5.62
CHEMBL3634329 1 5.51
CHEMBL1200606 MEXILETINE HYDROCHLORIDE 4.0 1 4.68
CHEMBL3634334 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3632695 IC50 = 670.0 nM 6.17
CHEMBL3634332 IC50 = 690.0 nM 6.16
CHEMBL3632698 IC50 = 2400.0 nM 5.62
CHEMBL3634329 IC50 = 3100.0 nM 5.51
CHEMBL1200606 MEXILETINE HYDROCHLORIDE IC50 = 21000.0 nM 4.68
CHEMBL3634334 IC50 = 34000.0 nM 4.47