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Assay Detail

CHEMBL715728

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Functional
In vitro functional potency using an automated assay employing LtK-cells stably expressing human recombinant mGlu5 receptor by measuring changes in cytosolic [Ca2+] concentration
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

[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor.
Cosford ND, Roppe J, Tehrani L, Schweiger EJ, Seiders TJ, Chaudary A, Rao S, Varney MA.
Bioorg Med Chem Lett (2003) 13 : 351 -354
PubMed 12565928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.62 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1169452 1 9.00
CHEMBL66654 1 8.70
CHEMBL1169453 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1169452 IC50 = 1.0 nM 9.00
CHEMBL66654 IC50 = 2.0 nM 8.70
CHEMBL1169453 IC50 = 7.0 nM 8.15