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ACS Med Chem Lett. 2014 Oct 23;6(1):73-8. doi: 10.1021/ml5003376. eCollection 2015 Jan 8.

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.

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Sanofi R&D , Industriepark Höchst Building G838, D-65926 Frankfurt am Main, Germany.
Leibniz-Institut für Molekulare Pharmakologie (FMP) , Robert-Rössle-Straße 10, 13125 Berlin-Buch, Germany.


From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chemistry and library approaches. This resulted in highly active small molecules with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure.


AGC kinase; Serum glucocorticoid regulated kinase; WNT signaling; virtual screening

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