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Assay Detail

CHEMBL828107

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

Binding
Displacement of [3H]AMPA from Ionotropic glutamate receptor of in rat brain synaptosomes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Convergent synthesis and pharmacology of substituted tetrazolyl-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid analogues.
Vogensen SB, Clausen RP, Greenwood JR, Johansen TN, Pickering DS, Nielsen B, Ebert B, Krogsgaard-Larsen P.
J Med Chem (2005) 48 : 3438 -3442
PubMed 15857151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.23 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370038 1 8.05
CHEMBL276815 (S)-AMPA 1 7.68
CHEMBL94859 1 7.57
CHEMBL370941 1 6.87
CHEMBL372643 1 5.60
CHEMBL193087 1 5.21
CHEMBL194226 1 4.57
CHEMBL317790 1 4.27
CHEMBL371784 1 -
CHEMBL363422 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370038 IC50 = 9.0 nM 8.05
CHEMBL276815 (S)-AMPA IC50 = 21.0 nM 7.68
CHEMBL94859 IC50 = 27.0 nM 7.57
CHEMBL370941 IC50 = 134.0 nM 6.87
CHEMBL372643 IC50 = 2500.0 nM 5.60
CHEMBL193087 IC50 = 6200.0 nM 5.21
CHEMBL194226 IC50 = 27000.0 nM 4.57
CHEMBL317790 IC50 = 54000.0 nM 4.27
CHEMBL371784 IC50 > 100000.0 nM -
CHEMBL363422 IC50 > 100000.0 nM -