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Assay Detail

CHEMBL3819955

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

Binding
Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Cell Type AZT
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium channel subfamily K member 2 (CHEMBL1075183)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?
Vivier D, Bennis K, Lesage F, Ducki S.
J Med Chem (2016) 59 : 5149 -5157
PubMed 26588045 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.84 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1491 AMLODIPINE 4.0 1 6.37
CHEMBL1275655 1 6.12
CHEMBL15848 ANANDAMIDE 1 6.00
CHEMBL30008 FLUNARIZINE 2.0 1 5.60
CHEMBL193 NIFEDIPINE 4.0 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1491 AMLODIPINE IC50 = 430.0 nM 6.37
CHEMBL1275655 IC50 = 750.0 nM 6.12
CHEMBL15848 ANANDAMIDE IC50 = 1000.0 nM 6.00
CHEMBL30008 FLUNARIZINE IC50 = 2500.0 nM 5.60
CHEMBL193 NIFEDIPINE IC50 = 8200.0 nM 5.09