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Assay Detail

CHEMBL4023249

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

Binding
Displacement of [3H]-LY459477 from mGlu2/3 receptor in Sprague-Dawley rat forebrain primary cortical membranes after 90 mins by liquid scintillation counting
2
Total Activities
2
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

Group II metabotropic glutamate receptor (mGlu2/mGlu3) (CHEMBL4106154)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist.
Monn JA, Henry SS, Massey SM, Clawson DK, Chen Q, Diseroad BA, Bhardwaj RM, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang XS, Carter JH, Getman BG, Adragni K, Broad LM, Sanger HE, Ursu D, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL, Hao J.
J Med Chem (2018) 61 : 2303 -2328
PubMed 29350927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.65 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081453 1 6.97
CHEMBL8759 EGLUMETAD 2.0 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081453 Ki = 106.0 nM 6.97
CHEMBL8759 EGLUMETAD Ki = 476.0 nM 6.32