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Assay Detail

CHEMBL697884

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

Binding
Binding affinity at Ionotropic glutamate receptor AMPA in rat cortical tissue by [3H]AMPA displacement.
18
Total Activities
18
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

Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution.
Ornstein PL, Arnold MB, Allen NK, Bleisch T, Borromeo PS, Lugar CW, Leander JD, Lodge D, Schoepp DD.
J Med Chem (1996) 39 : 2219 -2231
PubMed 8667365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.79 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308699 1 5.52
CHEMBL440869 1 5.38
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 5.32
CHEMBL71764 1 5.01
CHEMBL308941 1 4.89
CHEMBL71581 1 4.78
CHEMBL308563 1 4.64
CHEMBL446405 1 4.62
CHEMBL69614 1 4.24
CHEMBL71755 1 4.22
CHEMBL72123 1 4.07
CHEMBL71163 1 -
CHEMBL309097 1 -
CHEMBL406333 1 -
CHEMBL303600 1 -
CHEMBL303197 1 -
CHEMBL72655 1 -
CHEMBL305456 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308699 IC50 = 3000.0 nM 5.52
CHEMBL440869 IC50 = 4210.0 nM 5.38
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 4800.0 nM 5.32
CHEMBL71764 IC50 = 9800.0 nM 5.01
CHEMBL308941 IC50 = 12800.0 nM 4.89
CHEMBL71581 IC50 = 16800.0 nM 4.78
CHEMBL308563 IC50 = 23100.0 nM 4.64
CHEMBL446405 IC50 = 24000.0 nM 4.62
CHEMBL69614 IC50 = 57000.0 nM 4.24
CHEMBL71755 IC50 = 59600.0 nM 4.22
CHEMBL72123 IC50 = 84500.0 nM 4.07
CHEMBL71163 IC50 > 100000.0 nM -
CHEMBL309097 IC50 > 100000.0 nM -
CHEMBL406333 IC50 > 100000.0 nM -
CHEMBL303600 IC50 > 100000.0 nM -
CHEMBL303197 IC50 > 100000.0 nM -
CHEMBL72655 IC50 > 100000.0 nM -
CHEMBL305456 IC50 > 100000.0 nM -