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Assay Detail

CHEMBL4023242

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

Functional
Agonist activity at human mGlu6 receptor expressed in hamster AV12 cells co-expressing rat EAAT1 assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 6 (CHEMBL4573)
Type SINGLE PROTEIN
Organism Homo sapiens

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
EC50 1 5.71 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081453 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081453 EC50 = 1950.0 nM 5.71