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Assay Detail

CHEMBL862887

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

Binding
Displacement of [3H]MPEP from cloned human mGluR5 transfected in HEK293-T cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-T
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Iso Y, Grajkowska E, Wroblewski JT, Davis J, Goeders NE, Johnson KM, Sanker S, Roth BL, Tueckmantel W, Kozikowski AP.
J Med Chem (2006) 49 : 1080 -1100
PubMed 16451073 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.22 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201943 1 9.43
CHEMBL202307 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201943 Ki = 0.37 nM 9.43
CHEMBL202307 Ki = 1.003 nM 9.00