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Assay Detail

CHEMBL910641

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

Binding
Displacement of [125I]apamin from Wistar rat cortical apamin-sensitive site
8
Total Activities
8
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 methoxylated 1,2,3,4-tetrahydroisoquinolinium derivatives as ligands of the apamin-sensitive Ca2+-activated K+ channels.
Graulich A, Scuvée-Moreau J, Alleva L, Lamy C, Waroux O, Seutin V, Liégeois JF.
J Med Chem (2006) 49 : 7208 -7214
PubMed 17125273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.67 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215533 1 6.14
CHEMBL215029 1 6.04
CHEMBL215370 LAUDANOSINE METHIODIDE 1 5.89
CHEMBL215037 1 5.66
CHEMBL386836 1 5.44
CHEMBL214787 1 5.27
CHEMBL215382 1 5.24
CHEMBL525408 APAMIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215533 Ki = 730.0 nM 6.14
CHEMBL215029 Ki = 910.0 nM 6.04
CHEMBL215370 LAUDANOSINE METHIODIDE Ki = 1300.0 nM 5.89
CHEMBL215037 Ki = 2200.0 nM 5.66
CHEMBL386836 Ki = 3600.0 nM 5.44
CHEMBL214787 Ki = 5400.0 nM 5.27
CHEMBL215382 Ki = 5800.0 nM 5.24
CHEMBL525408 APAMIN Ki = 0.0038 nM -