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

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.