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Assay Detail

CHEMBL905113

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

Binding
Inhibition of rat potassium channel Kv2.1 by patch-clamp method
8
Total Activities
7
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

Potassium voltage-gated channel subfamily B member 1 (CHEMBL1075226)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.
Plouvier B, Beatch GN, Jung GL, Zolotoy A, Sheng T, Clohs L, Barrett TD, Fedida D, Wang WQ, Zhu JJ, Liu Y, Abraham S, Lynn L, Dong Y, Wall RA, Walker MJ.
J Med Chem (2007) 50 : 2818 -2841
PubMed 17506538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.40 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387935 1 5.62
CHEMBL229125 2 5.55
CHEMBL387671 1 5.50
CHEMBL375475 1 5.10
CHEMBL79 LIDOCAINE 4.0 1 -
CHEMBL652 FLECAINIDE 4.0 1 -
CHEMBL1294 QUINIDINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387935 IC50 = 2400.0 nM 5.62
CHEMBL229125 IC50 = 2800.0 nM 5.55
CHEMBL387671 IC50 = 3200.0 nM 5.50
CHEMBL229125 IC50 = 6000.0 nM 5.22
CHEMBL375475 IC50 = 8000.0 nM 5.10
CHEMBL79 LIDOCAINE IC50 - -
CHEMBL652 FLECAINIDE IC50 - -
CHEMBL1294 QUINIDINE IC50 - -