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Assay Detail

CHEMBL2050843

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

Binding
Displacement of [3H]glycine from NMDA receptor in rat cortical synaptical membrane
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

3-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.
Colotta V, Lenzi O, Catarzi D, Varano F, Squarcialupi L, Costagli C, Galli A, Ghelardini C, Pugliese AM, Maraula G, Coppi E, Pellegrini-Giampietro DE, Pedata F, Sabbadin D, Moro S.
Eur J Med Chem (2012) 54 : 470 -482
PubMed 22704999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.85 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 7.10
CHEMBL2047403 1 6.10
CHEMBL2047397 1 6.07
CHEMBL432748 1 5.96
CHEMBL2047398 1 5.89
CHEMBL2047404 1 5.29
CHEMBL2047399 1 5.21
CHEMBL2047401 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 Ki = 80.0 nM 7.10
CHEMBL2047403 Ki = 800.0 nM 6.10
CHEMBL2047397 Ki = 850.0 nM 6.07
CHEMBL432748 Ki = 1100.0 nM 5.96
CHEMBL2047398 Ki = 1300.0 nM 5.89
CHEMBL2047404 Ki = 5100.0 nM 5.29
CHEMBL2047399 Ki = 6100.0 nM 5.21
CHEMBL2047401 Ki = 6500.0 nM 5.19