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Assay Detail

CHEMBL702548

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

Binding
Compound was evaluated for inhibition of binding of [3H]AMPA to specific binding at Ionotropic glutamate receptor AMPA in rat cortical membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
Catarzi D, Colotta V, Varano F, Cecchi L, Filacchioni G, Galli A, Costagli C, Carlà V.
J Med Chem (2000) 43 : 3824 -3826
PubMed 11052786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.29 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 7.16
CHEMBL267276 TQX-173 1 6.85
CHEMBL314956 1 6.16
CHEMBL320952 1 6.01
CHEMBL310014 1 5.92
CHEMBL105895 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX Ki = 70.0 nM 7.16
CHEMBL267276 TQX-173 Ki = 140.0 nM 6.85
CHEMBL314956 Ki = 700.0 nM 6.16
CHEMBL320952 Ki = 980.0 nM 6.01
CHEMBL310014 Ki = 1200.0 nM 5.92
CHEMBL105895 Ki = 2300.0 nM 5.64