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Assay Detail

CHEMBL3768172

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

Binding
Displacement of [3H]MPEP from recombinant human mGluR5a expressed in A18 cells measured after 1 hr
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A18
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.
Galambos J, Domány G, Nógrádi K, Wágner G, Keserű GM, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Kóti J, Szakács Z, Béni Z, Gál K, Szombathelyi Z, Greiner I.
Bioorg Med Chem Lett (2016) 26 : 1249 -1252
PubMed 26774652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.53 7.77

Compounds Tested

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

Activity Data

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