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Assay Detail

CHEMBL884120

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Functional
AMPA receptor antagonistic activity as inhibition of depolarizations induced by 40 uM AMPA in rat cortical slice preparation
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
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 12 4.57 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 5.22
CHEMBL69614 1 4.56
CHEMBL446405 1 4.53
CHEMBL308941 1 4.39
CHEMBL303197 1 4.16
CHEMBL305456 1 -
CHEMBL71163 1 -
CHEMBL309097 1 -
CHEMBL406333 1 -
CHEMBL303600 1 -
CHEMBL72655 1 -
CHEMBL71755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14935 TEZAMPANEL ANHYDROUS IC50 = 6000.0 nM 5.22
CHEMBL69614 IC50 = 27600.0 nM 4.56
CHEMBL446405 IC50 = 29500.0 nM 4.53
CHEMBL308941 IC50 = 40900.0 nM 4.39
CHEMBL303197 IC50 = 69300.0 nM 4.16
CHEMBL305456 IC50 > 100000.0 nM -
CHEMBL71163 IC50 > 100000.0 nM -
CHEMBL309097 IC50 > 100000.0 nM -
CHEMBL406333 IC50 > 100000.0 nM -
CHEMBL303600 IC50 > 100000.0 nM -
CHEMBL72655 IC50 > 100000.0 nM -
CHEMBL71755 IC50 > 100000.0 nM -