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Assay Detail

CHEMBL746732

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

Binding
Inhibition of [3H]-MK-801 binding to a N-methyl-D-aspartic acid(NMDA) receptor in glycine-sensitive rat cortical membranes.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex.
McQuaid LA, Smith EC, Lodge D, Pralong E, Wikel JH, Calligaro DO, O'Malley PJ.
J Med Chem (1992) 35 : 3423 -3425
PubMed 1326635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.71 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116733 1 6.68
CHEMBL419940 1 6.26
CHEMBL50267 1 6.07
CHEMBL324519 1 5.14
CHEMBL299155 TRANSTORINE 1.0 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116733 IC50 = 210.0 nM 6.68
CHEMBL419940 IC50 = 550.0 nM 6.26
CHEMBL50267 IC50 = 860.0 nM 6.07
CHEMBL324519 IC50 = 7290.0 nM 5.14
CHEMBL299155 TRANSTORINE IC50 = 40200.0 nM 4.40