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Assay Detail

CHEMBL2382644

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

Functional
Antagonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by FLIPR assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type AV12
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 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
Monn JA, Valli MJ, Massey SM, Hao J, Reinhard MR, Bures MG, Heinz BA, Wang X, Carter JH, Getman BG, Stephenson GA, Herin M, Catlow JT, Swanson S, Johnson BG, McKinzie DL, Henry SS.
J Med Chem (2013) 56 : 4442 -4455
PubMed 23675965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.92 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381641 1 6.57
CHEMBL2381640 1 5.86
CHEMBL2381645 1 5.72
CHEMBL2381643 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381641 IC50 = 267.0 nM 6.57
CHEMBL2381640 IC50 = 1380.0 nM 5.86
CHEMBL2381645 IC50 = 1890.0 nM 5.72
CHEMBL2381643 IC50 = 3040.0 nM 5.52