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


ABSTRACT: To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules.Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies.Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds.The findings provide important tools for further study of this orphan G-protein coupled receptor.

SUBMITTER: Wang J 

PROVIDER: S-EPMC4648122 | biostudies-other | 2015 Jul

REPOSITORIES: biostudies-other

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