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Assay Detail

CHEMBL4053744

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

Binding
Displacement of [3H]M-MPEP from mGluR5 in rat cerebrocortical membranes measured after 60 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators.
Galambos J, Bielik A, Wágner G, Domány G, Kóti J, Béni Z, Szigetvári Á, Sánta Z, Orgován Z, Bobok A, Kiss B, Mikó-Bakk ML, Vastag M, Sághy K, Krasavin M, Gál K, Greiner I, Szombathelyi Z, Keserű GM.
Eur J Med Chem (2017) 133 : 240 -254
PubMed 28390229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.17 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765747 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765747 Ki = 68.0 nM 7.17