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Assay Detail

CHEMBL5336807

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

Binding
Inhibition of NO 711 marker binding to mouse GAT1 by LC-ESI-MS/MS based competitive MS binding assay
9
Total Activities
9
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
Ki 9 4.28 4.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5424877 1 4.61
CHEMBL5404846 1 4.55
CHEMBL5409309 1 4.39
CHEMBL5423316 1 4.34
CHEMBL5423337 1 4.24
CHEMBL5411369 1 4.17
CHEMBL5411905 1 4.11
CHEMBL5419680 1 4.10
CHEMBL5416293 1 4.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5424877 Ki = 24547.09 nM 4.61
CHEMBL5404846 Ki = 28183.83 nM 4.55
CHEMBL5409309 Ki = 40738.03 nM 4.39
CHEMBL5423316 Ki = 45708.82 nM 4.34
CHEMBL5423337 Ki = 57543.99 nM 4.24
CHEMBL5411369 Ki = 67608.3 nM 4.17
CHEMBL5411905 Ki = 77624.71 nM 4.11
CHEMBL5419680 Ki = 79432.82 nM 4.10
CHEMBL5416293 Ki = 93325.43 nM 4.03