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Assay Detail

CHEMBL2383450

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

Binding
Agonist activity at human mGlu2 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type AV12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 2 (CHEMBL5137)
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
EC50 13 7.88 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381640 1 9.80
CHEMBL2381652 1 9.25
CHEMBL2381641 1 8.89
CHEMBL2381642 1 8.12
CHEMBL2381643 1 8.12
CHEMBL2381644 1 8.09
CHEMBL2381645 1 7.91
CHEMBL2381647 1 7.67
CHEMBL365368 1 7.54
CHEMBL2381646 1 7.32
CHEMBL192051 1 7.20
CHEMBL2381649 1 6.59
CHEMBL2381651 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381640 EC50 = 0.16 nM 9.80
CHEMBL2381652 EC50 = 0.56 nM 9.25
CHEMBL2381641 EC50 = 1.3 nM 8.89
CHEMBL2381642 EC50 = 7.6 nM 8.12
CHEMBL2381643 EC50 = 7.5 nM 8.12
CHEMBL2381644 EC50 = 8.2 nM 8.09
CHEMBL2381645 EC50 = 12.2 nM 7.91
CHEMBL2381647 EC50 = 21.2 nM 7.67
CHEMBL365368 EC50 = 28.6 nM 7.54
CHEMBL2381646 EC50 = 47.9 nM 7.32
CHEMBL192051 EC50 = 63.6 nM 7.20
CHEMBL2381649 EC50 = 257.0 nM 6.59
CHEMBL2381651 EC50 = 1170.0 nM 5.93