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-Structure paper
Title | Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors. |
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Journal, issue, pages | J. Med. Chem., Vol. 55, Page 5291-5310, Year 2012 |
Publish date | Apr 6, 2012 (structure data deposition date) |
Authors | Ashwell, M.A. / Lapierre, J.M. / Brassard, C. / Bresciano, K. / Bull, C. / Cornell-Kennon, S. / Eathiraj, S. / France, D.S. / Hall, T. / Hill, J. ...Ashwell, M.A. / Lapierre, J.M. / Brassard, C. / Bresciano, K. / Bull, C. / Cornell-Kennon, S. / Eathiraj, S. / France, D.S. / Hall, T. / Hill, J. / Kelleher, E. / Khanapurkar, S. / Kizer, D. / Koerner, S. / Link, J. / Liu, Y. / Makhija, S. / Moussa, M. / Namdev, N. / Nguyen, K. / Nicewonger, R. / Palma, R. / Szwaya, J. / Tandon, M. / Uppalapati, U. / Vensel, D. / Volak, L.P. / Volckova, E. / Westlund, N. / Wu, H. / Yang, R.Y. / Chan, T.C. |
External links | J. Med. Chem. / PubMed:22533986 |
Methods | X-ray diffraction |
Resolution | 2.19 Å |
Structure data | PDB-4ejn: |
Chemicals | ChemComp-0R4: ChemComp-SBT: ChemComp-EDO: ChemComp-HOH: |
Source |
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Keywords | TRANSFERASE/TRANSFERASE INHIBITOR / Akt1 / autoinhibition / allosteric inhibitor / kinase inhibitor / hydrophobic collapase / Kinase / ATPase / TRANSFERASE-TRANSFERASE INHIBITOR complex |