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Assay Detail

CHEMBL895449

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

Binding
Blockade of SK channel in Wistar rat brain assessed as inhibition of apamin-sensitive after-hyperpolarisation
5
Total Activities
5
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 bis-isoquinolinium derivatives as small conductance Ca(2+)-activated K(+) channel blockers.
Graulich A, Dilly S, Farce A, Scuvée-Moreau J, Waroux O, Lamy C, Chavatte P, Seutin V, Liégeois JF.
J Med Chem (2007) 50 : 5070 -5075
PubMed 17867663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.32 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397282 1 5.62
CHEMBL394773 1 5.42
CHEMBL395568 1 5.39
CHEMBL242790 1 5.36
CHEMBL215370 LAUDANOSINE METHIODIDE 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397282 IC50 = 2400.0 nM 5.62
CHEMBL394773 IC50 = 3800.0 nM 5.42
CHEMBL395568 IC50 = 4100.0 nM 5.39
CHEMBL242790 IC50 = 4400.0 nM 5.36
CHEMBL215370 LAUDANOSINE METHIODIDE IC50 = 15000.0 nM 4.82