Xin Huang

Summary

Affiliation: Amgen Inc
Country: USA

Publications

  1. pmc A general joint model for longitudinal measurements and competing risks survival data with heterogeneous random effects
    Xin Huang
    Amgen Inc, 1120 Veterans Boulevard, Mail Stop ASF3 3, South San Francisco, CA 94080, USA
    Lifetime Data Anal 17:80-100. 2011
  2. ncbi request reprint Crystal structure of an inactive Akt2 kinase domain
    Xin Huang
    Amgen Cambridge Research Center, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Structure 11:21-30. 2003
  3. doi request reprint Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor
    Victor J Cee
    Department of Medicinal Chemistry, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142 and Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 53:6368-77. 2010
  4. doi request reprint 2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
    QingPing Zeng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 20:1652-6. 2010
  5. doi request reprint Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction
    John G Allen
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 52:7044-53. 2009
  6. doi request reprint Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase
    Victor J Cee
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Bldg 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 19:424-7. 2009
  7. doi request reprint Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation
    Erin F DiMauro
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1681-94. 2008
  8. doi request reprint Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity
    Matthew W Martin
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1637-48. 2008
  9. ncbi request reprint N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR
    Holly L Deak
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:1172-6. 2008
  10. ncbi request reprint Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR
    Erin F DiMauro
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 17:2305-9. 2007

Collaborators

Detail Information

Publications14

  1. pmc A general joint model for longitudinal measurements and competing risks survival data with heterogeneous random effects
    Xin Huang
    Amgen Inc, 1120 Veterans Boulevard, Mail Stop ASF3 3, South San Francisco, CA 94080, USA
    Lifetime Data Anal 17:80-100. 2011
    ..A Bayesian MCMC procedure is developed for parameter estimation and inference. Its performances and frequentist properties are investigated using simulations. A real data example is used to illustrate the usefulness of the approach...
  2. ncbi request reprint Crystal structure of an inactive Akt2 kinase domain
    Xin Huang
    Amgen Cambridge Research Center, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Structure 11:21-30. 2003
    ..Residues within the linker region between the N- and C-terminal lobes also contribute to the inactive conformation by partially occupying the ATP binding site...
  3. doi request reprint Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor
    Victor J Cee
    Department of Medicinal Chemistry, Amgen Inc, 360 Binney Street, Cambridge, Massachusetts 02142 and Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 53:6368-77. 2010
    ....
  4. doi request reprint 2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
    QingPing Zeng
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 20:1652-6. 2010
    ..Compound 30 was advanced to a mouse liver PD assay, where it showed dose-dependent inhibition of AKT activity, as measured by the inhibition of phospho-PRAS40...
  5. doi request reprint Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction
    John G Allen
    Chemistry Research and Discovery, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, USA
    J Med Chem 52:7044-53. 2009
    ..In cellular assays, these compounds were shown to upregulate p53 protein levels and p53 signaling and to cause p53-dependent inhibition of proliferation and apoptosis...
  6. doi request reprint Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase
    Victor J Cee
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Bldg 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 19:424-7. 2009
    ..Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase...
  7. doi request reprint Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation
    Erin F DiMauro
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1681-94. 2008
    ..Orally bioavailable compound 13b inhibited the anti-CD3-induced production of interleukin-2 (IL-2) in mice in a dose-dependent manner (ED 50 = 9.4 mg/kg)...
  8. doi request reprint Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity
    Matthew W Martin
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Cambridge, MA 02139, USA
    J Med Chem 51:1637-48. 2008
    ..This activity translates into inhibition of in vitro cell-based assays and in vivo models of T-cell activation and arthritis, respectively...
  9. ncbi request reprint N-(3-(phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: structure, synthesis and SAR
    Holly L Deak
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:1172-6. 2008
    ..X-ray co-crystal structural data, structure-activity relationships, and the synthesis of these inhibitors are reported herein...
  10. ncbi request reprint Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR
    Erin F DiMauro
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 17:2305-9. 2007
    ..Lead optimization was guided by X-ray crystallographic data, and preliminary SAR led to the identification of compounds with improved cellular potency and selectivity...
  11. ncbi request reprint Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties
    Matthew W Martin
    Department of Medicinal Chemistry, Amgen Inc, One Kendall Square, Building 1000, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 17:2299-304. 2007
    ..The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profiled to deduce their pharmacokinetic properties...
  12. ncbi request reprint Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity
    Erin F DiMauro
    Department of Medicinal Chemistry, Amgen, Inc, Cambridge, Massachusetts 02139, USA
    J Med Chem 49:5671-86. 2006
    ..Optimized, orally bioavailable compounds 32 and 47 exhibit anti-inflammatory activity (ED(50) of 22 and 11 mg/kg, respectively) in the anti-CD3-induced production of interleukin-2 (IL-2) in mice...
  13. ncbi request reprint Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity
    Matthew W Martin
    Department of Chemistry Research and Discovery, Amgen Inc, One Kendall Square, Building 1000, Cambridge, Massachusetts 02139, USA
    J Med Chem 49:4981-91. 2006
    ....
  14. doi request reprint Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors
    John L Buchanan
    Department of Medicinal Chemistry, Amgen Inc, 360 Binney Street, Cambridge, MA 02142, USA
    Bioorg Med Chem Lett 21:2394-9. 2011
    ..Herein, we report the synthesis, structure-activity relationships (SAR), X-ray cocrystal structure and in vivo tumor study results for a series of 2,4-bis-arylamino-1,3-pyrimidines...