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Assay Detail

CHEMBL833525

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

Binding
Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Metabotropic glutamate receptor 5 (CHEMBL2564)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists.
Nakazato A, Sakagami K, Yasuhara A, Ohta H, Yoshikawa R, Itoh M, Nakamura M, Chaki S.
J Med Chem (2004) 47 : 4570 -4587
PubMed 15317467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.94 4.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432038 1 4.94
CHEMBL186453 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432038 IC50 = 11400.0 nM 4.94
CHEMBL186453 IC50 = 11700.0 nM 4.93