GPRC6A is an L-amino acid sensing receptor with wide tissue expression and unknown physiological function. Using a chemogenomic approach we identified 3-substituted 2-phenyl-indoles 1  as allosteric modulators of GPRC6A. Potent allosteric modulators would be of value as pharmacological tools in vitro and in vivo. Synthesis routes to provide 2-5   and a wide range of analogues were developed, and a thorough structure-activity relationship study is currently underway, aiming at generating more potent and selective modulators of GPRC6A in the near future.

Taming the G protein-coupled receptor GPRC6A

245th National Meeting (2013)

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