Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2168304

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

Binding
Displacement of [3H]AZD9272 from mGluR5 in Sprague-Dawley rat striatum by autoradiographic analysis
2
Total Activities
2
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 and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.
Raboisson P, Breitholtz-Emanuelsson A, Dahllöf H, Edwards L, Heaton WL, Isaac M, Jarvie K, Kers A, Minidis AB, Nordmark A, Sheehan SM, Slassi A, Ström P, Terelius Y, Wensbo D, Wilson JM, Xin T, McLeod DA.
Bioorg Med Chem Lett (2012) 22 : 6974 -6979
PubMed 23046966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.73 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164552 1 7.84
CHEMBL2164538 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164552 IC50 = 14.5 nM 7.84
CHEMBL2164538 IC50 = 24.0 nM 7.62