(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.

  title={(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.},
  author={Jeffrey C. Pelletier and Joseph T Lundquist and A. M. Gilbert and Nipa Alon and Frederick J Bex and Bheem M Bhat and Mattew G Bursavich and Valerie E Coleburn and L. Arul Leo Felix and Daniel M Green and Paula D Green and Diane B Hauze and Yogendra P Kharode and H D Lam and Susan R Lockhead and Ronald L. Magolda and Jeanne J. Matteo and John F Mehlmann and Colleen F Milligan and Richard J Murrills and Jennifer Pirrello and Sally Selim and Michael C. Sharp and Ray Unwalla and Matthew D Vera and Jay E. Wrobel and Paul Yaworsky and Peter V. N. Bodine},
  journal={Journal of medicinal chemistry},
  volume={52 22},
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-to-lead in vitro optimization for target activity and molecular properties led to the discovery of (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine (5, WAY-262611). Compound 5 has excellent pharmacokinetic properties and showed a dose… CONTINUE READING
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