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Assay Detail

CHEMBL1059429

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

Binding
Displacement of [3H]KA from KA receptor in rat cortical synaptosomes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.
Clausen RP, Naur P, Kristensen AS, Greenwood JR, Strange M, Bräuner-Osborne H, Jensen AA, Nielsen AS, Geneser U, Ringgaard LM, Nielsen B, Pickering DS, Brehm L, Gajhede M, Krogsgaard-Larsen P, Kastrup JS.
J Med Chem (2009) 52 : 4911 -4922
PubMed 19588945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.17 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28472 1 5.80
CHEMBL553028 1 5.08
CHEMBL27130 1 4.64
CHEMBL276815 (S)-AMPA 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28472 IC50 = 1600.0 nM 5.80
CHEMBL553028 IC50 = 8300.0 nM 5.08
CHEMBL27130 IC50 = 23000.0 nM 4.64
CHEMBL276815 (S)-AMPA IC50 > 100000.0 nM -