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Assay Detail

CHEMBL5539608

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

Functional
Agonist activity at rat mGlu4 transfected in HEK293 cells co-transfected with chimeric Gqi9 incubated for 30 mins by IP-one HTRF assay
5
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 4 (CHEMBL2787)
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 5 6.98 7.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571283 2 7.45
CHEMBL33567 2 6.76
CHEMBL5570623 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571283 EC50 = 35.48 nM 7.45
CHEMBL5571283 EC50 = 110.0 nM 6.96
CHEMBL33567 EC50 = 173.78 nM 6.76
CHEMBL33567 EC50 = 180.0 nM 6.75
CHEMBL5570623 EC50 > 30000.0 nM -