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Assay Detail

CHEMBL681135

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

Binding
In vitro inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor from rat brain synaptic membranes.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions.
Brehm L, Krogsgaard-Larsen P, Schaumburg K, Johansen JS, Falch E, Curtis DR.
J Med Chem (1986) 29 : 224 -229
PubMed 3005567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.05 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307931 1 7.48
CHEMBL292757 1 4.82
CHEMBL309689 1 4.82
CHEMBL150830 1 4.14
CHEMBL309688 1 4.00
CHEMBL74364 1 -
CHEMBL305673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307931 IC50 = 33.0 nM 7.48
CHEMBL292757 IC50 = 15000.0 nM 4.82
CHEMBL309689 IC50 = 15000.0 nM 4.82
CHEMBL150830 IC50 = 72000.0 nM 4.14
CHEMBL309688 IC50 = 100000.0 nM 4.00
CHEMBL74364 IC50 > 100000.0 nM -
CHEMBL305673 IC50 > 100000.0 nM -