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Assay Detail

CHEMBL4008946

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

Binding
Displacement of [3H]M-MPEP from recombinant human mGluR5a expressed in human A18 cell membrane homogenate after 60 mins
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Metabotropic glutamate receptor 5 (CHEMBL3227)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 2 7.53 7.77
IC50 1 7.89 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765114 1 7.89
CHEMBL3764138 1 7.77
CHEMBL3765747 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765114 IC50 = 13.0 nM 7.89
CHEMBL3764138 Ki = 17.0 nM 7.77
CHEMBL3765747 Ki = 52.0 nM 7.28