James F Blake

Summary

Affiliation: Array BioPharma
Country: USA

Publications

  1. doi request reprint Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
    James F Blake
    Array BioPharma Inc, Boulder, CO 80301, USA Electronic address
    Bioorg Med Chem Lett 24:2635-9. 2014
  2. ncbi request reprint Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, USA
    J Med Chem 55:8110-27. 2012
  3. doi request reprint Discovery of pyrrolopyrimidine inhibitors of Akt
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 20:5607-12. 2010
  4. doi request reprint Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors
    Josef R Bencsik
    Array BioPharma Inc, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 20:7037-41. 2010
  5. doi request reprint Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA
    Rui Xu
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 21:2335-40. 2011
  6. doi request reprint Discovery and SAR of spirochromane Akt inhibitors
    Nicholas C Kallan
    Array BioPharma, Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 21:2410-4. 2011
  7. ncbi request reprint Examination of the computed molecular properties of compounds selected for clinical development
    James F Blake
    Array BioPharma, Boulder, CO, USA
    Biotechniques . 2003
  8. ncbi request reprint Integrating cheminformatic analysis in combinatorial chemistry
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, USA
    Curr Opin Chem Biol 8:407-11. 2004
  9. ncbi request reprint Structure-based generation of viable leads from small combinatorial libraries
    Ellen R Laird
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Curr Opin Drug Discov Devel 7:354-9. 2004
  10. doi request reprint Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2
    Li Ren
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, United States
    J Med Chem 58:1976-91. 2015

Collaborators

Detail Information

Publications14

  1. doi request reprint Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
    James F Blake
    Array BioPharma Inc, Boulder, CO 80301, USA Electronic address
    Bioorg Med Chem Lett 24:2635-9. 2014
    ..The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts. ..
  2. ncbi request reprint Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, USA
    J Med Chem 55:8110-27. 2012
    ..28 is currently being evaluated in human clinical trials for the treatment of cancer...
  3. doi request reprint Discovery of pyrrolopyrimidine inhibitors of Akt
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 20:5607-12. 2010
    ..The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts...
  4. doi request reprint Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors
    Josef R Bencsik
    Array BioPharma Inc, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 20:7037-41. 2010
    ..A representative dihydrothieno compound (34) was advanced into a PC3-NCI prostate mouse tumor model in which it demonstrated a dose-dependent reduction in tumor growth and stasis when dosed orally daily at 200 mg/kg...
  5. doi request reprint Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA
    Rui Xu
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 21:2335-40. 2011
    ..Representative compounds showed favorable Akt potency while exhibiting up to 1000-fold selectivity against PKA...
  6. doi request reprint Discovery and SAR of spirochromane Akt inhibitors
    Nicholas C Kallan
    Array BioPharma, Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Bioorg Med Chem Lett 21:2410-4. 2011
    ..Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA...
  7. ncbi request reprint Examination of the computed molecular properties of compounds selected for clinical development
    James F Blake
    Array BioPharma, Boulder, CO, USA
    Biotechniques . 2003
    ..The findings of this study provide guidance for combinatorial library design and lead selection, which may enhance the chance for ultimate success in lead optimization...
  8. ncbi request reprint Integrating cheminformatic analysis in combinatorial chemistry
    James F Blake
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, USA
    Curr Opin Chem Biol 8:407-11. 2004
    ..Awareness of the multi-objective nature of combinatorial library construction has also given rise to techniques designed to enhance the likelihood of including the best compounds in a given library...
  9. ncbi request reprint Structure-based generation of viable leads from small combinatorial libraries
    Ellen R Laird
    Array BioPharma Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Curr Opin Drug Discov Devel 7:354-9. 2004
    ..In this review, we will cover recent reports of small, focused libraries designed for specific therapeutic targets, and for which X-ray crystallographic data is available...
  10. doi request reprint Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2
    Li Ren
    Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, United States
    J Med Chem 58:1976-91. 2015
    ..On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation. ..
  11. ncbi request reprint Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
    C Todd Eary
    Array BioPharma, 3200 Walnut Street Boulder, CO 80301, USA
    Bioorg Med Chem Lett 17:2608-13. 2007
    ..This communication will describe the SAR and synthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors from early mu lead to advanced enantiomerically pure analogs...
  12. ncbi request reprint Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo
    Kurtis D Davies
    Cell Biology, Array BioPharma, Inc, Boulder, CO 80301, USA
    Oncol Res 19:349-63. 2011
    ..Together, these results suggest that single-agent inhibition of Chk1 may be an effective treatment strategy for selected human malignancies...
  13. ncbi request reprint Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones
    Eli M Wallace
    Array BioPharma, Boulder, Colorado 80301, USA
    J Med Chem 49:441-4. 2006
    ..These inhibitors exhibit excellent cellular potency and good pharmacokinetic properties and have demonstrated the ability to inhibit ERK phosphorylation in HT-29 tumors from mouse xenograft studies...
  14. ncbi request reprint Identification and evaluation of molecular properties related to preclinical optimization and clinical fate
    James F Blake
    Array BioPharma, Inc, 3200 Walnut Street, Boulder, CO 80301, USA
    Med Chem 1:649-55. 2005
    ..Finally, emerging data suggests that there has been a shift in the leading causes of compound attrition, and attention should now be focused on building toxicological models to guide drug discovery efforts...