Research Topics
| James F BlakeSummaryAffiliation: Array BioPharma Country: USA Publications
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Detail Information
Publications
Examination of the computed molecular properties of compounds selected for clinical developmentJames 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...- Identification and evaluation of molecular properties related to preclinical optimization and clinical fateJames 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... - Integrating cheminformatic analysis in combinatorial chemistryJames 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... - Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKARui 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... - Discovery and SAR of spirochromane Akt inhibitorsNicholas 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... - Structure-based generation of viable leads from small combinatorial librariesEllen 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... - Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitorsJosef 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... - Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivoKurtis 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... - Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitorsC 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... - Discovery of pyrrolopyrimidine inhibitors of AktJames 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... - Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-onesEli 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... - Consensus scoring for ligand/protein interactionsRobert D Clark
Tripos Inc, St Louis, MO 63144, USA
J Mol Graph Model 20:281-95. 2002..We find that the reliability and interpretability of results can be improved by combining results from all four functions into a CScore...