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Assay Detail

CHEMBL699888

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

Binding
Compound was tested for in vitro binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA ligand
8
Total Activities
8
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 (CHEMBL2096617)
Type PROTEIN COMPLEX GROUP
Organism Mus musculus

Publication

Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)propionic acid.
Johansen TN, Ebert B, Bräuner-Osborne H, Didriksen M, Christensen IT, Søby KK, Madsen U, Krogsgaard-Larsen P, Brehm L.
J Med Chem (1998) 41 : 930 -939
PubMed 9526567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.25 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL279956 QUISQUALATE 1 7.10
CHEMBL71073 1 6.47
CHEMBL315663 1 6.32
CHEMBL73698 1 6.22
CHEMBL10339 1 5.75
CHEMBL73069 1 4.50
CHEMBL173847 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL279956 QUISQUALATE IC50 = 80.0 nM 7.10
CHEMBL71073 IC50 = 340.0 nM 6.47
CHEMBL315663 IC50 = 480.0 nM 6.32
CHEMBL73698 IC50 = 600.0 nM 6.22
CHEMBL10339 IC50 = 1800.0 nM 5.75
CHEMBL73069 IC50 = 32000.0 nM 4.50
CHEMBL173847 IC50 > 1000000.0 nM -