Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.

  title={Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-\{[(3S)-3-piperidinylmethyl]oxy\}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.},
  author={Dirk A. Heerding and Nelson Rhodes and Jack D Leber and Tammy J Clark and Richard M Keenan and Louis V Lafrance and Mei Li and Igor Safonov and Dennis T Takata and Joseph W Venslavsky and Dennis S. Yamashita and Anthony E. Choudhry and Robert A Copeland and Zhihong Lai and Michael D. Schaber and Peter J. Tummino and Susan L Strum and Edgar R. Wood and Derek R. Duckett and Derek J. Eberwein and Victoria B Knick and Timothy J Lansing and RANDY T. MCCONNELL and Shuyun Zhang and Elisabeth A. Minthorn and Nestor O. Concha and Gregory L. Warren and Rakesh Kumar},
  journal={Journal of medicinal chemistry},
  volume={51 18},
Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of dominant negative AKT blocks the ability of a variety of growth factors to promote survival. Therefore, inhibitors of AKT kinase activity might be useful as monotherapy for the treatment of tumors with activated AKT. Herein, we describe our lead optimization studies… CONTINUE READING