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Assay Detail

CHEMBL1913010

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

Binding
Displacement of [125I]-apamin from cloned SK3 channel expressed in human HEK293 cells after 1 hr by liquid scintillation counting
5
Total Activities
5
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

Publication

Synthesis and radioligand binding studies of bis-(8-isopropyl-isoquinolinium) derivatives as ligands for apamin-sensitive sites on cloned SK2 and SK3 channels.
Badarau E, Dilly S, Dufour F, Poncin S, Seutin V, Liégeois JF.
Bioorg Med Chem Lett (2011) 21 : 6756 -6759
PubMed 21978678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.45 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1909931 1 7.34
CHEMBL1909929 1 6.67
CHEMBL1909930 1 6.24
CHEMBL1909928 1 6.08
CHEMBL1909932 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1909931 Ki = 46.0 nM 7.34
CHEMBL1909929 Ki = 214.0 nM 6.67
CHEMBL1909930 Ki = 575.0 nM 6.24
CHEMBL1909928 Ki = 837.0 nM 6.08
CHEMBL1909932 Ki = 1268.0 nM 5.90