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.