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Assay Detail

CHEMBL4019819

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

Functional
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP level
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 4 (CHEMBL2736)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4.
Charvin D, Pomel V, Ortiz M, Frauli M, Scheffler S, Steinberg E, Baron L, Deshons L, Rudigier R, Thiarc D, Morice C, Manteau B, Mayer S, Graham D, Giethlen B, Brugger N, Hédou G, Conquet F, Schann S.
J Med Chem (2017) 60 : 8515 -8537
PubMed 28902994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.38 7.16
Emax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067875 1 7.16
CHEMBL507522 1 5.60
CHEMBL4089083 FOLIGLURAX 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067875 EC50 = 70.0 nM 7.16
CHEMBL507522 EC50 = 2500.0 nM 5.60
CHEMBL4089083 FOLIGLURAX Emax = 70.0 % -