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TitleSyntheses of Potent, Selective, and Orally Bioavailable Indazole-Pyridine Series of Protein Kinase B/Akt Inhibitors with Reduced Hypotension.
Journal, issue, pagesJ. Med. Chem., Vol. 50, Page 2990-, Year 2007
Publish dateMay 1, 2007 (structure data deposition date)
AuthorsZhu, G.D. / Gandhi, V.B. / Gong, J. / Thomas, S. / Woods, K.W. / Song, X. / Li, T. / Diebold, R.B. / Luo, Y. / Liu, X. ...Zhu, G.D. / Gandhi, V.B. / Gong, J. / Thomas, S. / Woods, K.W. / Song, X. / Li, T. / Diebold, R.B. / Luo, Y. / Liu, X. / Guan, R. / Klinghofer, V. / Johnson, E.F. / Bouska, J. / Olson, A. / Marsh, K.C. / Stoll, V.S. / Mamo, M. / Polakowski, J. / Campbell, T.J. / Martin, R.L. / Gintant, G.A. / Penning, T.D. / Li, Q. / Rosenberg, S.H. / Giranda, V.L.
External linksJ. Med. Chem. / PubMed:17523610
MethodsX-ray diffraction
Resolution2.1 - 2.5 Å
Structure data

PDB-2uzt:
PKA structures of AKT, indazole-pyridine inhibitors
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

PDB-2uzu:
PKA structures of indazole-pyridine series of AKT inhibitors
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

PDB-2uzv:
PKA structures of indazole-pyridine series of AKT inhibitors
Method: X-RAY DIFFRACTION / Resolution: 2.5 Å

PDB-2uzw:
PKA structures of indazole-pyridine series of AKT inhibitors
Method: X-RAY DIFFRACTION / Resolution: 2.2 Å

Chemicals

ChemComp-SS3:
(2S)-1-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}-3-PHENYLPROPAN-2-AMINE

ChemComp-L20:
(2S)-1-(1H-INDOL-3-YL)-3-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}PROPAN-2-AMINE

ChemComp-SS5:
(2S)-1-[3-(CYCLOHEXYLMETHOXY)PHENYL]-3-{[5-(3-METHYL-1H-INDAZOL-5-YL)PYRIDIN-3-YL]OXY}PROPAN-2-AMINE

ChemComp-SS4:
3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO[1,2-.C.] PYRAZOLE

Source
  • bos taurus (domestic cattle)
KeywordsTRANSFERASE / CAMP / KINASE / MYRISTATE / LIPOPROTEIN / SERINE/THREONINE-PROTEIN KINASE / PHOSPHORYLATION / PROTEIN KINASE A / NUCLEOTIDE-BINDING / PROTEIN KINASE INHIBITOR / ATP- BINDING / AKT INHIBITORS / NUCLEAR PROTEIN / ATP-BINDING

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