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Assay Detail

CHEMBL910532

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

Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type RGT
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Metabotropic glutamate receptor 3 (CHEMBL2888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
Monn JA, Massey SM, Valli MJ, Henry SS, Stephenson GA, Bures M, Hérin M, Catlow J, Giera D, Wright RA, Johnson BG, Andis SL, Kingston A, Schoepp DD.
J Med Chem (2007) 50 : 233 -240
PubMed 17228865 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.79 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218710 2 9.77
CHEMBL8839 LY-389795 1 8.33
CHEMBL275079 LY-379268 1 8.24
CHEMBL375611 LY404039 1.0 1 7.04
CHEMBL8759 EGLUMETAD 2.0 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218710 Ki = 0.17 nM 9.77
CHEMBL8839 LY-389795 Ki = 4.7 nM 8.33
CHEMBL275079 LY-379268 Ki = 5.8 nM 8.24
CHEMBL375611 LY404039 Ki = 92.0 nM 7.04
CHEMBL8759 EGLUMETAD Ki = 93.3 nM 7.03
CHEMBL218710 Ki = 447.0 nM 6.35