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Assay Detail

CHEMBL833280

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Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu2 receptor
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
Dominguez C, Prieto L, Valli MJ, Massey SM, Bures M, Wright RA, Johnson BG, Andis SL, Kingston A, Schoepp DD, Monn JA.
J Med Chem (2005) 48 : 3605 -3612
PubMed 15887967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.14 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8759 EGLUMETAD 2.0 1 8.00
CHEMBL365368 1 7.35
CHEMBL192051 2 6.79
CHEMBL195500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8759 EGLUMETAD EC50 = 10.0 nM 8.00
CHEMBL365368 EC50 = 45.0 nM 7.35
CHEMBL192051 EC50 = 161.0 nM 6.79
CHEMBL192051 EC50 = 397.0 nM 6.40
CHEMBL195500 EC50 > 100000.0 nM -