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Assay Detail

CHEMBL874051

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

Functional
Concentration necessary for 50% inhibition of depolarization induced by 5 uM NMDA in mouse cortical wedge preparation
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Intermediate

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
Catarzi D, Colotta V, Varano F, Calabri FR, Filacchioni G, Galli A, Costagli C, Carlà V.
J Med Chem (2004) 47 : 262 -272
PubMed 14695840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.39 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 5.33
CHEMBL267276 TQX-173 1 4.34
CHEMBL328935 1 4.30
CHEMBL91115 1 4.30
CHEMBL90722 1 4.28
CHEMBL90242 1 4.22
CHEMBL91677 1 4.22
CHEMBL328272 1 4.10
CHEMBL93076 1 -
CHEMBL222519 NBQX 1 -
CHEMBL327894 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 IC50 = 4700.0 nM 5.33
CHEMBL267276 TQX-173 IC50 = 46000.0 nM 4.34
CHEMBL328935 IC50 = 50000.0 nM 4.30
CHEMBL91115 IC50 = 50000.0 nM 4.30
CHEMBL90722 IC50 = 52000.0 nM 4.28
CHEMBL90242 IC50 = 60000.0 nM 4.22
CHEMBL91677 IC50 = 60000.0 nM 4.22
CHEMBL328272 IC50 = 80000.0 nM 4.10
CHEMBL93076 IC50 - nM -
CHEMBL222519 NBQX IC50 - nM -
CHEMBL327894 IC50 = 150000.0 nM -