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Assay Detail

CHEMBL2169528

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

Functional
Antagonist activity at KCNQ1 expressed in CHO cells incubated for 3 mins by automated patch clamp assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Potassium voltage-gated channel subfamily KQT member 1 (CHEMBL1866)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Cheung YY, Yu H, Xu K, Zou B, Wu M, McManus OB, Li M, Lindsley CW, Hopkins CR.
J Med Chem (2012) 55 : 6975 -6979
PubMed 22793372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.54 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164048 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164048 IC50 = 2920.0 nM 5.54