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Assay Detail

CHEMBL702516

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

Binding
Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as a radioligand
7
Total Activities
5
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 (CHEMBL2096670)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.
Ornstein PL, Arnold MB, Allen NK, Leander JD, Tizzano JP, Lodge D, Schoepp DD.
J Med Chem (1995) 38 : 4885 -4890
PubMed 8523401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.88 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 5.32
CHEMBL308941 3 5.24
CHEMBL72123 1 4.07
CHEMBL144462 1 -
CHEMBL423201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 4800.0 nM 5.32
CHEMBL308941 IC50 = 5700.0 nM 5.24
CHEMBL308941 IC50 = 12800.0 nM 4.89
CHEMBL72123 IC50 = 84500.0 nM 4.07
CHEMBL308941 IC50 > 100000.0 nM -
CHEMBL144462 IC50 > 100000.0 nM -
CHEMBL423201 IC50 > 100000.0 nM -