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Assay Detail

CHEMBL4371741

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

Binding
Inhibition of mouse GAT4 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

GABA transporter 4 (CHEMBL3699)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.
Hauke TJ, Wein T, Höfner G, Wanner KT.
J Med Chem (2018) 61 : 10310 -10332
PubMed 30376325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.44 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526583 1 4.82
CHEMBL4436249 1 4.38
CHEMBL4525620 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526583 IC50 = 15135.61 nM 4.82
CHEMBL4436249 IC50 = 41686.94 nM 4.38
CHEMBL4525620 IC50 = 75857.76 nM 4.12