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Assay Detail

CHEMBL5114467

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

Binding
Inhibition of [3H]-GABA uptake at GAT-1 in rat forebrain synaptosomes assessed as inhibition constant preincubated for 8 mins followed by [3H]-GABA addition measured after 8 mins by scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Forebrain
Subcellular Synaptosomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium- and chloride-dependent GABA transporter 1 (CHEMBL4054)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 1 7.85 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5205864 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5205864 Ki = 14.0 nM 7.85