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Assay Detail

CHEMBL807622

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

Binding
In vitro inhibition of [3H]GABA uptake at the Sodium- and chloride-dependent GABA transporter 1 (GAT-1) uptake site in rat brain synaptosomes
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Synaptosomes
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.
Knutsen LJ, Andersen KE, Lau J, Lundt BF, Henry RF, Morton HE, Naerum L, Petersen H, Stephensen H, Suzdak PD, Swedberg MD, Thomsen C, Sørensen PO.
J Med Chem (1999) 42 : 3447 -3462
PubMed 10479278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.36 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542207 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542207 Ki = 440.0 nM 6.36