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Assay Detail

CHEMBL830165

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

Binding
Inhibition of [125I]apamin binding to calcium-activated potassium (SK) channel of rat cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Small conductance calcium-activated potassium channel (CHEMBL2096673)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and radioligand binding studies of C-5- and C-8-substituted 1-(3,4-dimethoxybenzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums as SK channel blockers related to N-methyl-laudanosine and N-methyl-noscapine.
Graulich A, Scuvée-Moreau J, Seutin V, Liégeois JF.
J Med Chem (2005) 48 : 4972 -4982
PubMed 16033276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.68 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365744 1 5.07
CHEMBL215370 LAUDANOSINE METHIODIDE 1 5.06
CHEMBL186011 1 4.87
CHEMBL190220 1 4.85
CHEMBL525408 APAMIN 1 4.69
CHEMBL190992 1 4.59
CHEMBL188644 1 4.55
CHEMBL187736 1 4.45
CHEMBL427162 1 4.40
CHEMBL190003 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365744 IC50 = 8600.0 nM 5.07
CHEMBL215370 LAUDANOSINE METHIODIDE IC50 = 8700.0 nM 5.06
CHEMBL186011 IC50 = 13600.0 nM 4.87
CHEMBL190220 IC50 = 14100.0 nM 4.85
CHEMBL525408 APAMIN IC50 = 20400.0 nM 4.69
CHEMBL190992 IC50 = 25400.0 nM 4.59
CHEMBL188644 IC50 = 28400.0 nM 4.55
CHEMBL187736 IC50 = 35200.0 nM 4.45
CHEMBL427162 IC50 = 39600.0 nM 4.40
CHEMBL190003 IC50 = 50000.0 nM 4.30