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Assay Detail

CHEMBL5506733

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Functional
Agonist activity at rat mGluR2 receptor expressed in HEK293 cells by IP-1 HTRF assay
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 2 (CHEMBL2851)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological characterization of conformationally restricted 2-amino-Adipic acid analogs and carboxycyclopropyl glycines as selective metabotropic glutamate 2 receptor agonists.
Staudt M, Liu N, Malhaire F, Doroudian Y, Prézeau L, Renard E, Hasanpour Z, Pin JP, Bunch L.
Eur J Med Chem (2024) 266 : 116157 -116157
PubMed 38245976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.07 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275079 LY-379268 2 9.22
CHEMBL5532032 2 7.09
CHEMBL5555290 2 5.75
CHEMBL5560070 2 5.39
CHEMBL5558260 2 5.12
CHEMBL5517920 2 5.05
CHEMBL5537101 2 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275079 LY-379268 EC50 = 0.6 nM 9.22
CHEMBL275079 LY-379268 EC50 = 0.6166 nM 9.21
CHEMBL5532032 EC50 = 82.0 nM 7.09
CHEMBL5532032 EC50 = 81.28 nM 7.09
CHEMBL5555290 EC50 = 1798.0 nM 5.75
CHEMBL5555290 EC50 = 1819.7 nM 5.74
CHEMBL5560070 EC50 = 4100.0 nM 5.39
CHEMBL5560070 EC50 = 4073.8 nM 5.39
CHEMBL5558260 EC50 = 7500.0 nM 5.12
CHEMBL5558260 EC50 = 7585.78 nM 5.12
CHEMBL5517920 EC50 = 8900.0 nM 5.05
CHEMBL5517920 EC50 = 8912.51 nM 5.05
CHEMBL5537101 EC50 = 10000.0 nM 5.00
CHEMBL5537101 EC50 = 15848.93 nM 4.80