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Assay Detail

CHEMBL681952

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

Binding
In vitro binding affinity against Gamma-aminobutyric acid A receptor in rat brain synaptic membranes at pH 7.1
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline.
Nielsen L, Brehm L, Krogsgaard-Larsen P.
J Med Chem (1990) 33 : 71 -77
PubMed 2153214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.74 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.48
CHEMBL351355 1 6.70
CHEMBL349005 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 33.0 nM 7.48
CHEMBL351355 IC50 = 200.0 nM 6.70
CHEMBL349005 IC50 = 900.0 nM 6.05