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Assay Detail

CHEMBL1059435

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

Binding
Displacement of [3H]AMPA from rat recombinant GluR1 flop isoform expressed in baculovirus infected Sf9 cells
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

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
Ki 3 6.00 6.63
pKi 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28472 2 6.63
CHEMBL553028 2 5.81
CHEMBL27130 2 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28472 Ki = 232.0 nM 6.63
CHEMBL553028 Ki = 1550.0 nM 5.81
CHEMBL27130 Ki = 2780.0 nM 5.56
CHEMBL27130 pKi = 3.526 nM -
CHEMBL28472 pKi = 2.364 nM -
CHEMBL553028 pKi = 3.177 nM -