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For Akt enzyme assay details and the proposed model for the allosteric mode of inhibition of these inhibitors, see: Barnett, S. F.; Defeo-Jones, D.; Fu, S.; Hancock, P. J.; Haskell, K. M.; Jones, R. E.; Kahana, J. A.; Kral, A.; Leander, K.; Lee, L. L.; Malinowski, J.; McAvoy, E. M.; Nahas, D. D.; Robinson, R.; Huber, H. E. Biochemistry, in press
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Compounds 9,13, and 16 were obtained from the Merck internal sample collection
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note
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Similar behavior was observed with a carboxylate in the 5-position, which was alleviated when the corresponding methyl ester analog was tested, providing further evidence of zwitterionic character affording poor cell permeability in this series
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