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Assay Detail

CHEMBL715727

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Functional
In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated phosphoinositide (PI) hydrolysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
Gasparini F, Andres H, Flor PJ, Heinrich M, Inderbitzin W, Lingenhöhl K, Müller H, Munk VC, Omilusik K, Stierlin C, Stoehr N, Vranesic I, Kuhn R.
Bioorg Med Chem Lett (2002) 12 : 407 -409
PubMed 11814808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.99 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112677 1 8.00
CHEMBL66654 1 7.44
CHEMBL88612 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112677 IC50 = 10.0 nM 8.00
CHEMBL66654 IC50 = 36.0 nM 7.44
CHEMBL88612 IC50 = 3000.0 nM 5.52