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Assay Detail

CHEMBL5116583

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

Binding
Agonist activity at Kv7.4 (unknown origin) expressed in CHO cells co-expressing GFP
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium voltage-gated channel subfamily KQT member 4 (CHEMBL3576)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of an automated screen for Kv7.2 potassium channels and discovery of a new agonist chemotype.
Hernandez CC, Tarfa RA, Miguel I Limcaoco J, Liu R, Mondal P, Hill C, Keith Duncan R, Tzounopoulos T, Stephenson CRJ, O'Meara MJ, Wipf P.
Bioorg Med Chem Lett (2022) 71 : 128841 -128841
PubMed 35671848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.45 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5185685 1 7.06
CHEMBL5200636 1 6.50
CHEMBL4549229 1 6.18
CHEMBL4458793 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5185685 EC50 = 87.0 nM 7.06
CHEMBL5200636 EC50 = 320.0 nM 6.50
CHEMBL4549229 EC50 = 660.0 nM 6.18
CHEMBL4458793 EC50 = 910.0 nM 6.04