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Assay Detail

CHEMBL2060190

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

Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
8
Total Activities
8
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

Α-amino-β-fluorocyclopropanecarboxylic acids as a new tool for drug development: synthesis of glutamic acid analogs and agonist activity towards metabotropic glutamate receptor 4.
Lemonnier G, Lion C, Quirion JC, Pin JP, Goudet C, Jubault P.
Bioorg Med Chem (2012) 20 : 4716 -4726
PubMed 22750138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.51 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33567 1 6.89
CHEMBL2058378 1 6.47
CHEMBL575060 GLUTAMIC ACID 3.0 1 5.54
CHEMBL2058382 1 4.56
CHEMBL2058381 1 4.07
CHEMBL2058379 1 -
CHEMBL2058380 1 -
CHEMBL2058383 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33567 EC50 = 130.0 nM 6.89
CHEMBL2058378 EC50 = 340.0 nM 6.47
CHEMBL575060 GLUTAMIC ACID EC50 = 2880.0 nM 5.54
CHEMBL2058382 EC50 = 27400.0 nM 4.56
CHEMBL2058381 EC50 = 85600.0 nM 4.07
CHEMBL2058379 EC50 = 609000.0 nM -
CHEMBL2058380 EC50 = 465000.0 nM -
CHEMBL2058383 EC50 = 1400000.0 nM -