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Assay Detail

CHEMBL697360

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

Binding
In vitro binding affinity against Ionotropic glutamate receptor AMPA binding site using [3H]- AMPA as radioligand on rat cortical synaptosomal membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Design and synthesis of novel quinoxaline-2,3-dione AMPA/GlyN receptor antagonists: amino acid derivatives.
Nikam SS, Cordon JJ, Ortwine DF, Heimbach TH, Blackburn AC, Vartanian MG, Nelson CB, Schwarz RD, Boxer PA, Rafferty MF.
J Med Chem (1999) 42 : 2266 -2271
PubMed 10377233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.28 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293206 1 7.20
CHEMBL431382 1 6.85
CHEMBL73704 1 5.93
CHEMBL75761 1 5.80
CHEMBL307667 1 5.63
CHEMBL419638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293206 IC50 = 63.0 nM 7.20
CHEMBL431382 IC50 = 140.0 nM 6.85
CHEMBL73704 IC50 = 1180.0 nM 5.93
CHEMBL75761 IC50 = 1590.0 nM 5.80
CHEMBL307667 IC50 = 2320.0 nM 5.63
CHEMBL419638 IC50 > 10000.0 nM -