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Assay Detail

CHEMBL701234

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

Binding
Binding affinity of compound was determined against Ionotropic glutamate receptor AMPA receptor, using radioligand [3H]- AMPA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glutamate receptor 1 (CHEMBL3753)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).
Bjerrum EJ, Kristensen AS, Pickering DS, Greenwood JR, Nielsen B, Liljefors T, Schousboe A, Bräuner-Osborne H, Madsen U.
J Med Chem (2003) 46 : 2246 -2249
PubMed 12747796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.75 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL72366 1 6.66
CHEMBL73698 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL72366 IC50 = 220.0 nM 6.66
CHEMBL73698 IC50 = 650.0 nM 6.19