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Assay Detail

CHEMBL781143

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

Functional
Concentration giving 50% inhibition of stimulated [3H](+)-MK-801 binding in rat cortical membranes incubated with 10 uM glycine
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

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 4.64 4.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91115 1 4.96
CHEMBL328272 1 4.90
CHEMBL90242 1 4.54
CHEMBL267276 TQX-173 1 4.17
CHEMBL90722 1 -
CHEMBL328935 1 -
CHEMBL93076 1 -
CHEMBL222519 NBQX 1 -
CHEMBL327894 1 -
CHEMBL50267 1 -
CHEMBL91677 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91115 IC50 = 11000.0 nM 4.96
CHEMBL328272 IC50 = 12700.0 nM 4.90
CHEMBL90242 IC50 = 29000.0 nM 4.54
CHEMBL267276 TQX-173 IC50 = 68000.0 nM 4.17
CHEMBL90722 IC50 - nM -
CHEMBL328935 IC50 - nM -
CHEMBL93076 IC50 - nM -
CHEMBL222519 NBQX IC50 - nM -
CHEMBL327894 IC50 - nM -
CHEMBL50267 IC50 - nM -
CHEMBL91677 IC50 - nM -