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Acta Pharmacol Sin. 2015 Jul;36(7):874-8. doi: 10.1038/aps.2015.12. Epub 2015 Jun 1.

High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139.

Author information

1
The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
2
Neuroscience Drug Discovery, H Lundbeck A/S, DK-2500 Copenhagen, Denmark.

Abstract

AIM:

To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules.

METHODS:

Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies.

RESULTS:

Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds.

CONCLUSION:

The findings provide important tools for further study of this orphan G-protein coupled receptor.

PMID:
26027661
PMCID:
PMC4648122
DOI:
10.1038/aps.2015.12
[Indexed for MEDLINE]
Free PMC Article

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