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Assay Detail

CHEMBL4031692

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

Binding
Inhibition of mouse GAT1 expressed in hamster BHK cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method
1
Total Activities
1
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

Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
Jørgensen L, Al-Khawaja A, Kickinger S, Vogensen SB, Skovgaard-Petersen J, Rosenthal E, Borkar N, Löffler R, Madsen KK, Bräuner-Osborne H, Schousboe A, Ecker GF, Wellendorph P, Clausen RP.
J Med Chem (2017) 60 : 8834 -8846
PubMed 28991462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 4.72 4.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1446457 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1446457 Ki = 19000.0 nM 4.72