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Assay Detail

CHEMBL5539607

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

Functional
Agonist activity at rat mGlu3 transfected in HEK293 cells co-transfected with chimeric Gqi9 incubated for 30 mins by IP-one HTRF assay
6
Total Activities
3
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 3 (CHEMBL3067)
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 6 6.72 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275079 LY-379268 2 8.00
CHEMBL5571283 2 6.43
CHEMBL5570623 2 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275079 LY-379268 EC50 = 10.0 nM 8.00
CHEMBL275079 LY-379268 EC50 = 10.0 nM 8.00
CHEMBL5571283 EC50 = 375.0 nM 6.43
CHEMBL5571283 EC50 = 371.54 nM 6.43
CHEMBL5570623 EC50 = 1880.0 nM 5.73
CHEMBL5570623 EC50 = 1862.09 nM 5.73