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Assay Detail

CHEMBL697372

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

Binding
Ability of compound to displace [3H]AMPA from Ionotropic glutamate receptor AMPA in rat cerebral cortex synaptic membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Colotta V, Catarzi D, Varano F, Calabri FR, Filacchioni G, Costagli C, Galli A.
Bioorg Med Chem Lett (2004) 14 : 2345 -2349
PubMed 15081038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.39 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310286 1 6.60
CHEMBL432748 1 5.89
CHEMBL311831 1 5.01
CHEMBL307267 1 5.01
CHEMBL80594 1 4.94
CHEMBL77569 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310286 Ki = 250.0 nM 6.60
CHEMBL432748 Ki = 1300.0 nM 5.89
CHEMBL311831 Ki = 9700.0 nM 5.01
CHEMBL307267 Ki = 9800.0 nM 5.01
CHEMBL80594 Ki = 11600.0 nM 4.94
CHEMBL77569 Ki = 12500.0 nM 4.90