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Assay Detail

CHEMBL5114476

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

Binding
Inhibition of mouse GAT-1 assessed as inhibition of GABA uptake
2
Total Activities
2
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

Nipecotic acid as potential lead molecule for the development of GABA uptake inhibitors; structural insights and design strategies.
Singh K, Kumar P, Bhatia R, Mehta V, Kumar B, Akhtar MJ.
Eur J Med Chem (2022) 234 : 114269 -114269
PubMed 35306287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.36 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207397 1 7.43
CHEMBL5178760 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207397 IC50 = 37.15 nM 7.43
CHEMBL5178760 IC50 = 52.48 nM 7.28