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

  • Acta Pharmacol Sin. 2015 Jul;36(7):874-8. doi: 10.1038/aps.2015.12.
Jia Wang  1 ,  Lin-yun Zhu  1 ,  Qing Liu  1 ,  Morten Hentzer  2 ,  Garrick Paul Smith  2 ,  Ming-wei Wang  1
Affiliations
  • 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.
PMID: 26027661 DOI: 10.1038/aps.2015.12
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.

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