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Assay Detail

CHEMBL4715625

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

Binding
Inhibition of mouse Nav1.7 alpha expressed in HEK293 cells incubated for 5 mins measured after hyperpolarization to -115 mV for 8s followed by 20ms pulse with holding potential of -20 mV by PatchXpress automated patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
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

Discovery of Arylsulfonamide Na1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ,Layton ME,Pero JE,Kelly MJ,Greshock TJ,Kraus RL,Li Y,Klein R,Clements M,Daley C,Jovanovska A,Ballard JE,Wang D,Zhao F,Brunskill APJ,Peng X,Wang X,Sun H,Houghton AK,Burgey CS
ACS Med Chem Lett (2021) 12 : 1038 -1049
PubMed 34141090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.12 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062780 1 6.66
CHEMBL4061793 1 6.41
CHEMBL4090731 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062780 IC50 = 220.0 nM 6.66
CHEMBL4061793 IC50 = 390.0 nM 6.41
CHEMBL4090731 IC50 = 5000.0 nM 5.30