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Assay Detail

CHEMBL4255620

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

Binding
Inhibition of Nav1.7 (unknown origin) expressed in HEK293 cells at -60 mV holding potential measured after 600 secs by patch clamp method
8
Total Activities
8
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

Acyl Sulfonamides NaV1.7 Blockers Useful for the Treatment of Pain.
Blass BE.
ACS Med Chem Lett (2018) 9 : 161 -162
PubMed 29541350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.23 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4290933 1 7.80
CHEMBL4276864 1 7.42
CHEMBL4292013 1 7.31
CHEMBL4287506 1 7.23
CHEMBL4280298 1 7.18
CHEMBL4283748 1 7.07
CHEMBL4279180 1 7.05
CHEMBL4294322 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4290933 IC50 = 16.0 nM 7.80
CHEMBL4276864 IC50 = 38.0 nM 7.42
CHEMBL4292013 IC50 = 49.0 nM 7.31
CHEMBL4287506 IC50 = 59.0 nM 7.23
CHEMBL4280298 IC50 = 66.0 nM 7.18
CHEMBL4283748 IC50 = 86.0 nM 7.07
CHEMBL4279180 IC50 = 90.0 nM 7.05
CHEMBL4294322 IC50 = 154.0 nM 6.81