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Assay Detail

CHEMBL753044

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

Functional
Inhibition of veratridine-induced Na+ influx in chinese hamster ovary cells expressing alpha subunit of rat brain type voltage-gated sodium channel type 2
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Cell Type ovary
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium channel protein type 2 subunit alpha (CHEMBL3399)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.
Roufos I, Hays SJ, Dooley DJ, Schwarz RD, Campbell GW, Probert AW.
J Med Chem (1994) 37 : 268 -274
PubMed 8295214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.19 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30008 FLUNARIZINE 2.0 1 6.38
CHEMBL92870 LIDOFLAZINE 2.0 1 5.62
CHEMBL282833 1 5.57
CHEMBL93106 1 5.51
CHEMBL92018 1 5.46
CHEMBL313859 1 5.44
CHEMBL330049 1 5.37
CHEMBL327859 1 5.35
CHEMBL92071 1 5.24
CHEMBL92977 1 5.24
CHEMBL92918 1 5.12
CHEMBL93436 1 4.92
CHEMBL329245 1 4.89
CHEMBL93634 1 4.89
CHEMBL91288 1 4.54
CHEMBL93838 1 4.50
CHEMBL91929 1 4.14
CHEMBL93065 1 -
CHEMBL94137 1 -
CHEMBL93271 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30008 FLUNARIZINE IC50 = 420.0 nM 6.38
CHEMBL92870 LIDOFLAZINE IC50 = 2400.0 nM 5.62
CHEMBL282833 IC50 = 2700.0 nM 5.57
CHEMBL93106 IC50 = 3100.0 nM 5.51
CHEMBL92018 IC50 = 3500.0 nM 5.46
CHEMBL313859 IC50 = 3600.0 nM 5.44
CHEMBL330049 IC50 = 4300.0 nM 5.37
CHEMBL327859 IC50 = 4500.0 nM 5.35
CHEMBL92071 IC50 = 5800.0 nM 5.24
CHEMBL92977 IC50 = 5700.0 nM 5.24
CHEMBL92918 IC50 = 7500.0 nM 5.12
CHEMBL93436 IC50 = 12000.0 nM 4.92
CHEMBL329245 IC50 = 13000.0 nM 4.89
CHEMBL93634 IC50 = 13000.0 nM 4.89
CHEMBL91288 IC50 = 29000.0 nM 4.54
CHEMBL93838 IC50 = 32000.0 nM 4.50
CHEMBL91929 IC50 = 72000.0 nM 4.14
CHEMBL93065 IC50 > 100000.0 nM -
CHEMBL94137 IC50 = 106000.0 nM -
CHEMBL93271 IC50 > 100000.0 nM -