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Assay Detail

CHEMBL5336847

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

Binding
Inhibition of mouse GAT1
6
Total Activities
5
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

Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445)
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 6 5.54 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1190271 2 6.52
CHEMBL2403791 1 5.05
CHEMBL5431496 1 4.89
CHEMBL5430628 1 4.72
CHEMBL3403559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1190271 IC50 = 300.0 nM 6.52
CHEMBL1190271 IC50 = 309.03 nM 6.51
CHEMBL2403791 IC50 = 9000.0 nM 5.05
CHEMBL5431496 IC50 = 13000.0 nM 4.89
CHEMBL5430628 IC50 = 19000.0 nM 4.72
CHEMBL3403559 IC50 = 562341.33 nM -