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Assay Detail

CHEMBL698529

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

Binding
Ability to displace [3H]-kainic acid radioligand at kainate receptor in rat cortical membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, kainate (CHEMBL2094119)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.
Brehm L, Greenwood JR, Hansen KB, Nielsen B, Egebjerg J, Stensbøl TB, Bräuner-Osborne H, Sløk FA, Kronborg TT, Krogsgaard-Larsen P.
J Med Chem (2003) 46 : 1350 -1358
PubMed 12672235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.10 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28472 1 5.80
CHEMBL29024 1 4.85
CHEMBL27130 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28472 IC50 = 1600.0 nM 5.80
CHEMBL29024 IC50 = 14000.0 nM 4.85
CHEMBL27130 IC50 = 23000.0 nM 4.64