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Assay Detail

CHEMBL752501

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

Binding
Ability of compound to displace [3H]glycine from N-methyl-D-aspartate glutamate receptor 1 from in cerebral cortex synaptic membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
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 7 5.90 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307267 1 6.70
CHEMBL80594 1 6.62
CHEMBL77569 1 6.52
CHEMBL432748 1 5.96
CHEMBL311831 1 4.97
CHEMBL77362 1 4.64
CHEMBL310286 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307267 Ki = 200.0 nM 6.70
CHEMBL80594 Ki = 240.0 nM 6.62
CHEMBL77569 Ki = 300.0 nM 6.52
CHEMBL432748 Ki = 1100.0 nM 5.96
CHEMBL311831 Ki = 10600.0 nM 4.97
CHEMBL77362 Ki = 23000.0 nM 4.64
CHEMBL310286 Ki > 100000.0 nM -