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Assay Detail

CHEMBL5539615

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

Functional
Agonist activity at SNAP tagged rat mGlu2 transfected HEK293 cells preincubated with antagonist LY-341495 followed by compound addition by TR-FRET assay
2
Total Activities
2
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

Design, Synthesis, Pharmacology, and In Silico Studies of (1<i>S</i>,2<i>S</i>,3<i>S</i>)-2-((<i>S</i>)-Amino(carboxy)methyl)-3-(carboxymethyl)cyclopropane-1-carboxylic Acid (LBG30300): A Picomolar Potency Subtype-Selective mGlu<sub>2</sub> Receptor Agonist.
Liu N, Eshak F, Malhaire F, Brabet I, Prézeau L, Renard E, Pin JP, Acher FC, Staudt M, Bunch L.
J Med Chem (2024) 67 : 1314 -1326
PubMed 38170918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.15 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571283 1 7.66
CHEMBL8759 EGLUMETAD 2.0 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571283 EC50 = 22.0 nM 7.66
CHEMBL8759 EGLUMETAD EC50 = 229.0 nM 6.64