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Assay Detail

CHEMBL5336848

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

Binding
Inhibition of mouse GAT2
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

GABA transporter 2 (CHEMBL4228)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Zaręba P, Łątka K, Mazur G, Gryzło B, Pasieka A, Godyń J, Panek D, Skrzypczak-Wiercioch A, Höfner GC, Latacz G, Maj M, Espargaró A, Sabaté R, Jóźwiak K, Wanner KT, Sałat K, Malawska B, Kulig K, Bajda M.
Eur J Med Chem (2023) 261 : 115832 -115832
PubMed 37837674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.87 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5431496 1 5.22
CHEMBL5430628 1 4.89
CHEMBL3403559 2 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5431496 IC50 = 6000.0 nM 5.22
CHEMBL5430628 IC50 = 13000.0 nM 4.89
CHEMBL3403559 IC50 = 21000.0 nM 4.68
CHEMBL3403559 IC50 = 21379.62 nM 4.67