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Assay Detail

CHEMBL2405424

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

Binding
Inhibition of GABA uptake at murine BGT-1 expressed in HEK293 cells
8
Total Activities
8
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 2 (CHEMBL4228)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis of N-substituted acyclic β-amino acids and their investigation as GABA uptake inhibitors.
Sitka I, Allmendinger L, Fülep G, Höfner G, Wanner KT.
Eur J Med Chem (2013) 65 : 487 -499
PubMed 23770450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.47 4.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75035 1 4.51
CHEMBL2403781 1 4.42
CHEMBL1995111 1 -
CHEMBL297569 BETA-ALANINE 1 -
CHEMBL38686 1 -
CHEMBL77484 (S)-NIPECOTIC ACID 1 -
CHEMBL77575 (R)-NIPECOTIC ACID 1 -
CHEMBL277498 NIPECOTIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75035 IC50 = 30902.95 nM 4.51
CHEMBL2403781 IC50 = 38018.94 nM 4.42
CHEMBL1995111 IC50 = 812830.52 nM -
CHEMBL297569 BETA-ALANINE IC50 = 331131.12 nM -
CHEMBL38686 IC50 = 371535.23 nM -
CHEMBL77484 (S)-NIPECOTIC ACID IC50 = 758577.58 nM -
CHEMBL77575 (R)-NIPECOTIC ACID IC50 = 524807.46 nM -
CHEMBL277498 NIPECOTIC ACID IC50 = 794328.23 nM -