Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors

Burdick, Daniel J.; Wang, Shumei; Heise, Christopher; Pan, Borlan; Drummond, Jake; Yin, JianPing; Goeser, Lauren; Magnuson, Steven; Blaney, Jeff; Moffat, John; Wang, Weiru; Chen, Huifen

doi:10.1016/j.bmcl.2015.08.048

Title: Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors

Authors:: Burdick, Daniel J.; Wang, Shumei; Heise, Christopher; Pan, Borlan; Drummond, Jake; Yin, JianPing; Goeser, Lauren; Magnuson, Steven; Blaney, Jeff; Moffat, John; Wang, Weiru; Chen, Huifen

Publication Date:: Sun Nov 01 00:00:00 EDT 2015

Sponsoring Org.:: USDOE Office of Science (SC), Basic Energy Sciences (BES)

OSTI Identifier:: 1250395

Grant/Contract Number:: AC02-05CH11231

Resource Type:: Publisher's Accepted Manuscript

Journal Name:: Bioorganic and Medicinal Chemistry Letters

Additional Journal Information:: Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Volume: 25 Journal Issue: 21; Journal ID: ISSN 0960-894X

Publisher:: Elsevier

Country of Publication:: United Kingdom

Language:: English

Citation Formats


                    Burdick, Daniel J., Wang, Shumei, Heise, Christopher, Pan, Borlan, Drummond, Jake, Yin, JianPing, Goeser, Lauren, Magnuson, Steven, Blaney, Jeff, Moffat, John, Wang, Weiru, and Chen, Huifen. Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.  United Kingdom: N. p., 2015. 
Web.  doi:10.1016/j.bmcl.2015.08.048.

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                    Burdick, Daniel J., Wang, Shumei, Heise, Christopher, Pan, Borlan, Drummond, Jake, Yin, JianPing, Goeser, Lauren, Magnuson, Steven, Blaney, Jeff, Moffat, John, Wang, Weiru, & Chen, Huifen. Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.  United Kingdom.  https://doi.org/10.1016/j.bmcl.2015.08.048

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                    Burdick, Daniel J., Wang, Shumei, Heise, Christopher, Pan, Borlan, Drummond, Jake, Yin, JianPing, Goeser, Lauren, Magnuson, Steven, Blaney, Jeff, Moffat, John, Wang, Weiru, and Chen, Huifen. Sun .  
"Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors".  United Kingdom.  https://doi.org/10.1016/j.bmcl.2015.08.048.

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@article{osti_1250395,

  title        = {Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors},

  author       = {Burdick, Daniel J. and Wang, Shumei and Heise, Christopher and Pan, Borlan and Drummond, Jake and Yin, JianPing and Goeser, Lauren and Magnuson, Steven and Blaney, Jeff and Moffat, John and Wang, Weiru and Chen, Huifen},

  abstractNote = {},

  doi          = {10.1016/j.bmcl.2015.08.048},

  journal      = {Bioorganic and Medicinal Chemistry Letters},

  number       = 21,

  volume       = 25,

  place        = {United Kingdom},

  year         = {Sun Nov 01 00:00:00 EDT 2015},

  month        = {Sun Nov 01 00:00:00 EDT 2015}

}

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https://doi.org/10.1016/j.bmcl.2015.08.048

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Works referenced in this record:

Targeting the RAF–MEK–ERK pathway in cancer therapy
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Title: Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors

Citation Formats

Targeting the RAF–MEK–ERK pathway in cancer therapy journal, October 2009

Ligand efficiency: a useful metric for lead selection journal, May 2004

Group Epitope Mapping by Saturation Transfer Difference NMR To Identify Segments of a Ligand in Direct Contact with a Protein Receptor journal, June 2001

9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation journal, August 2009

Ligand efficiency indices for effective drug discovery journal, April 2007

Synthesis, Biological Testing, and Binding Mode Prediction of 6,9-Diarylpurin-8-ones as p38 MAP Kinase Inhibitors journal, May 2007

Recent Developments in Anti-Cancer Agents Targeting the Ras/Raf/ MEK/ERK Pathway journal, January 2009

Cross-coupling reactions via organoboranes journal, July 2002

Targeting the RAF–MEK–ERK pathway in cancer therapy
journal, October 2009

Ligand efficiency: a useful metric for lead selection
journal, May 2004

Group Epitope Mapping by Saturation Transfer Difference NMR To Identify Segments of a Ligand in Direct Contact with a Protein Receptor
journal, June 2001

9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation
journal, August 2009

Ligand efficiency indices for effective drug discovery
journal, April 2007

Synthesis, Biological Testing, and Binding Mode Prediction of 6,9-Diarylpurin-8-ones as p38 MAP Kinase Inhibitors
journal, May 2007

Recent Developments in Anti-Cancer Agents Targeting the Ras/Raf/ MEK/ERK Pathway
journal, January 2009

Cross-coupling reactions via organoboranes
journal, July 2002