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Assay Detail

CHEMBL4008959

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

Functional
Negative allosteric modulation of mGluR5 in E17 Sprague-Dawley rat primary neuronal cultures assessed as reduction of DHPG-induced cytosolic Ca2+ influx after 10 to 20 mins by fluo-4/AM-dye based fluorometric analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Galambos J, Bielik A, Krasavin M, Orgován Z, Domány G, Nógrádi K, Wágner G, Balogh GT, Béni Z, Kóti J, Szakács Z, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Laszy J, Halász AS, Balázs O, Gál K, Greiner I, Szombathelyi Z, Keserű GM.
J Med Chem (2017) 60 : 2470 -2484
PubMed 28212015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.72 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765114 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765114 IC50 = 19.0 nM 7.72