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Assay Detail

CHEMBL4056904

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

Binding
Inhibition of rat NaV1.7 at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress automated 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 5.25 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100413 1 5.39
CHEMBL4076051 1 5.31
CHEMBL4076380 1 5.25
CHEMBL4100514 1 5.03
CHEMBL4071906 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100413 IC50 = 4100.0 nM 5.39
CHEMBL4076051 IC50 = 4900.0 nM 5.31
CHEMBL4076380 IC50 = 5600.0 nM 5.25
CHEMBL4100514 IC50 = 9400.0 nM 5.03
CHEMBL4071906 IC50 > 30000.0 nM -