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Assay Detail

CHEMBL909970

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

Binding
Displacement of [3H]glycine from Gly/NMDA receptor in rat cortical synaptic 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

Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Colotta V, Catarzi D, Varano F, Lenzi O, Filacchioni G, Costagli C, Galli A, Ghelardini C, Galeotti N, Gratteri P, Sgrignani J, Deflorian F, Moro S.
J Med Chem (2006) 49 : 6015 -6026
PubMed 17004715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.91 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80594 1 6.62
CHEMBL385438 1 6.00
CHEMBL385648 1 4.64
CHEMBL217826 1 4.60
CHEMBL386418 1 4.38
CHEMBL218290 1 4.06
CHEMBL217073 1 4.05
CHEMBL387049 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80594 Ki = 240.0 nM 6.62
CHEMBL385438 Ki = 1000.0 nM 6.00
CHEMBL385648 Ki = 22700.0 nM 4.64
CHEMBL217826 Ki = 25000.0 nM 4.60
CHEMBL386418 Ki = 42000.0 nM 4.38
CHEMBL218290 Ki = 88000.0 nM 4.06
CHEMBL217073 Ki = 90000.0 nM 4.05
CHEMBL387049 Ki > 30000.0 nM -