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Assay Detail

CHEMBL4056903

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

Binding
Inhibition of slow inactivated rat NaV1.7 at -20 mV holding potential after 5 mins by IonWorks electrophysiology method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.
Schenkel LB, DiMauro EF, Nguyen HN, Chakka N, Du B, Foti RS, Guzman-Perez A, Jarosh M, La DS, Ligutti J, Milgram BC, Moyer BD, Peterson EA, Roberts J, Yu VL, Weiss MM.
Bioorg Med Chem Lett (2017) 27 : 3817 -3824
PubMed 28684121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.40 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100514 1 7.64
CHEMBL4076051 1 7.62
CHEMBL4100413 1 7.37
CHEMBL4071906 1 7.31
CHEMBL4076380 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100514 IC50 = 23.0 nM 7.64
CHEMBL4076051 IC50 = 24.0 nM 7.62
CHEMBL4100413 IC50 = 43.0 nM 7.37
CHEMBL4071906 IC50 = 49.0 nM 7.31
CHEMBL4076380 IC50 = 88.0 nM 7.06