Original Article

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

Jia Wang, Lin-yun Zhu, Qing Liu, Morten Hentzer, Garrick Paul Smith, Ming-wei Wang
DOI: 10.1038/aps.2015.12


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.
Keywords: orphan G-protein coupled receptor; GPR139; high-throughput screening; calcium mobilization assay; antagonist

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