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Assay Detail

CHEMBL909976

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

Functional
Antagonist activity against AMPA receptor assessed as inhibition of SAMPA-induced depolarization of mouse cortex
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2096617)
Type PROTEIN COMPLEX GROUP
Organism Mus musculus

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
IC50 3 5.83 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 6.70
CHEMBL217826 1 5.46
CHEMBL310286 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX IC50 = 200.0 nM 6.70
CHEMBL217826 IC50 = 3500.0 nM 5.46
CHEMBL310286 IC50 = 4600.0 nM 5.34