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Assay Detail

CHEMBL752329

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

Binding
Binding affinity in rat brain cortical membranes by the displacement of [3H]- DCKA at N-methyl-D-aspartate glutamate receptor 1
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Cai SX, Huang JC, Espitia SA, Tran M, Ilyin VI, Hawkinson JE, Woodward RM, Weber E, Keana JF.
J Med Chem (1997) 40 : 3679 -3686
PubMed 9357535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.84 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123196 1 6.16
CHEMBL333042 1 6.00
CHEMBL91801 1 5.98
CHEMBL123885 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123196 IC50 = 690.0 nM 6.16
CHEMBL333042 IC50 = 1000.0 nM 6.00
CHEMBL91801 IC50 = 1050.0 nM 5.98
CHEMBL123885 IC50 = 5900.0 nM 5.23