Contents

• Year 3 Reports
  • Identification of Inhibitors of Trypanosoma brucei Hexokinases
    Elizabeth Sharlow, Jennifer E Golden, Heidi Dodson, Meredith Morris, Marcia Hesser, Todd Lyda, Stephanie Leimgruber, Chad E Schroeder, Dan P Flaherty, Warren S Weiner, Denise Simpson, John S Lazo, Jeffrey Aubé, and James C Morris.
    Received: December 15, 2010; Last Update: June 24, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Novel Chemical Inhibitor of TRPC4 Channels
    Melissa R. Miller, Jie Shi, Meng Wu, Julie Engers, Corey R. Hopkins, Craig W. Lindsley, James M. Salovich, Yingmin Zhu, Jin-Bin Tian, Michael X. Zhu, Owen B. McManus, and Min Li.
    Received: December 15, 2010; Last Update: May 26, 2011.
    • Probe Structure & Characteristics
    • Recommendations for Scientific Use of the Probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendix
  • Screening for Selective Ligands for GPR55 - Antagonists
    Susanne Heynen-Genel, Russell Dahl, Shenghua Shi, Loribelle Milan, Santosh Hariharan, Eduard Sergienko, Michael Hedrick, Shakeela Dad, Derek Stonich, Ying Su, Michael Vicchiarelli, Arianna Mangravita-Novo, Layton H Smith, Thomas DY Chung, Haleli Sharir, Marc G Caron, Lawrence S Barak, and Mary E Abood.
    Received: October 30, 2010; Last Update: May 26, 2011.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Center Summary of Results
    • 3 Probe Optimization
    • 4 Probe
    • 5 Comparative data showing probe specificity for target in biologically relevant assays
    • Bibliography
  • Antagonist for the Kappa Opioid Receptor
    Michael P Hedrick, Palak Gosalia, Kelin Li, Kevin J Frankowski, Shenghua Shi, Thomas E Prisinzano, Frank Schoenen, Jeffrey Aubé, Ying Su, Derek Stonich, Stefan Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Loribelle Milan, Susanne Heynen-Genel, Michael Vicchiarelli, Arianna Mangravita-Novo, John M Streicher, Layton H Smith, Thomas DY Chung, Marc Caron, Laura M Bohn, and Lawrence S Barak.
    Received: October 31, 2010; Last Update: May 26, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix Synthetic procedures and compound characterization
  • Identification of Small Molecule Inhibitors that Suppress Cytokine-Induced Apoptosis in Human Pancreatic Islet Cells
    Patrick W Faloon, Danny Hung-Chieh Chou, Erin M Forbeck, Deepika Walpita, Barbara Morgan, Sara Buhrlage, Amal Ting, Jose Perez, Lawrence J MacPherson, Jeremy R Duvall, Sivaraman Dandapani, Lisa A Marcaurelle, Ben Munoz, Michelle Palmer, Michael Foley, Bridget Wagner, and Stuart L Schreiber.
    Received: October 29, 2010; Last Update: May 26, 2011.
    • Probe Structure and Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and LC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • Screening for Selective Ligands for GPR55 - Agonists
    Susanne Heynen-Genel, Russell Dahl, Shenghua Shi, Loribelle Milan, Santosh Hariharan, Yalda Bravo, Eduard Sergienko, Michael Hedrick, Shakeela Dad, Derek Stonich, Ying Su, Michael Vicchiarelli, Arianna Mangravita-Novo, Layton H Smith, Thomas DY Chung, Haleli Sharir, Lawrence S Barak, and Mary E Abood.
    Received: September 29, 2010; Last Update: May 26, 2011.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Center Summary of Results
    • 3 Probe Optimization
    • 4 Probe
    • 5 Comparative data showing probe specificity for target in biologically relevant assays
    • Bibliography
• Year 2 Reports
  • Discovery, SAR and Biological Evaluation of Aryl-thiazol-piperidines as SMN Modulators
    Jingbo Xiao, Juan J Marugan, Wei Zheng, Steve Titus, Noel Southall, Jonathan J Cherry, Matthew Evans, Elliot J Androphy, and Christopher P Austin.
    Received: March 19, 2010; Last Update: May 5, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Antagonists of IAP-family anti-apoptotic proteins - Probe 2
    Marcos Lopez, Kate Welsh, Hongbin Yuan, Derek Stonich, Ying Su, Xochella Garcia, Michael Cuddy, Richard Houghten, Eduard Sergienko, John C Reed, Robert Ardecky, Santhi Reddy, Darren Finlay, Kristiina Vuori, Shakeela Dad, Thomas DY Chung, and Nicholas DP Cosford.
    Received: September 1, 2009; Last Update: February 10, 2011.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Identification of activators for the M2 isoform of human pyruvate kinase Version 3
    Matthew B Boxer, Jian-kang Jiang, Matthew G Vander Heiden, Min Shen, Henrike Veith, Lewis C Cantley, and Craig J Thomas.
    Received: September 1, 2009; Last Update: March 3, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of these probes
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • Probe properties
    • 5 References
  • Discovery and development of a second highly selective M₁ Positive Allosteric Modulator (PAM)
    Thomas M Bridges, Paul R Reid, L Michelle Lewis, Eric S Dawson, C David Weaver, Michael R Wood, and Craig W Lindsley.
    Received: March 31, 2010; Last Update: October 29, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Bibliography
    • Appendix I Solubility, Stability and Reactivity data as determined by Absorption Systems
    • Appendix II Liquid Chromatography-Mass Spectrometry (LCMS) and Nuclear Magnetic Resonance (NMR) as prepared by Vanderbilt Specialized Chemistry Center
  • Identification of compounds which inhibit cytotoxicity associated with mutant Huntingtin protein expression
    Steve Titus, Natalie Elia, Noel Southall, Wei Zheng, Juan Jose Marugan, and Marcy MacDonald.
    Received: March 30, 2010; Last Update: March 11, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • An inhibitor of the Cdc2-like kinase 4 (Clk4)
    Andrew S Rosenthal, Cordelle Tanega, Min Shen, Bryan T Mott, James M Bougie, Dac-Trung Nguyen, Tom Misteli, Douglas S Auld, David J Maloney, and Craig J Thomas.
    Received: March 29, 2010; Last Update: March 3, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • Probe properties
    • 5 References
  • Inhibitors of Platelet Integrin αllbβ3
    Josh McCoy, Min Shen, Wenwei Huang, Barry Coller, and Craig J Thomas.
    Received: March 27, 2010; Last Update: March 3, 2011.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Identification of Small-Molecule Inhibitors of Trypansoma cruzi Infection - Probe 1
    Leigh C Carmody, Andrew Germain, Douglas Barker, Cristina Galan-Rodriguez, Esther Bettiol, Ana Rodriguez, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: March 26, 2010; Last Update: March 11, 2011.
    • Probe Structure and Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and LC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • Identification of a small molecule that selectively activates alpha-synuclein translational expression
    Nathan T Ross, Shailesh R Metkar, Hanh Le, Jason Burbank, Catherine Cahill, Andrew Germain, Lawrence MacPherson, Joshua Bittker, Michelle Palmer, Jack Rogers, and Stuart L Schreiber.
    Received: February 4, 2011; Last Update: February 15, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
  • Screen for RAS-Selective Lethal Compounds and VDAC Ligands - Probe 1
    Joshua A Bittker, Michel Weiwer, Kenichi Shimada, Wan S Yang, Lawrence MacPherson, Sivaraman Dandapani, Ben Munoz, Michelle Palmer, Brent R Stockwell, and Stuart L Schreiber.
    Received: March 26, 2010; Last Update: February 10, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
  • Chemical Genetic Analysis of Platelet Granule Secretion-Probe 3
    Lynn VerPlank, Chris Dockendorff, Joseph Negri, Jose R Perez, James Dilks, Lawrence MacPherson, Michelle Palmer, Robert Flaumenhaft, and Stuart L Schreiber.
    Received: March 25, 2010; Last Update: February 10, 2011.
    • Probe Structure and Characteristics
    • Recommendations for Scientific Use of the Probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
    • Acknowledgements
  • Chemical Genetic Analysis of Platelet Granule Secretion-Probe 2
    Lynn VerPlank, Chris Dockendorff, Joseph Negri, Jose R Perez, James Dilks, Lawrence MacPherson, Michelle Palmer, Robert Flaumenhaft, and Stuart L Schreiber.
    Received: March 25, 2010; Last Update: February 10, 2011.
    • Probe Structure and Characteristics
    • Recommendations for Scientific Use of the Probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
    • Acknowledgements
  • Chemical Genetic Analysis of Platelet Granule Secretion-Probe 1
    Lynn VerPlank, Chris Dockendorff, Joseph Negri, Jose R Perez, James Dilks, Lawrence MacPherson, Michelle Palmer, Robert Flaumenhaft, and Stuart L Schreiber.
    Received: March 25, 2010; Last Update: February 10, 2011.
    • Probe Structure and Characteristics
    • Recommendations for Scientific Use of the Probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Acknowledgements
    • Appendices
  • Identification of Small-Molecule Inhibitors of Trypansoma cruzi Infection - Probe 3
    Leigh C Carmody, Andrew Germain, Douglas Barker, Cristina Galan-Rodriguez, Esther Bettiol, Ana Rodriguez, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: March 25, 2010; Last Update: March 11, 2011.
    • Probe Structure and Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and LC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • Identification of Small-Molecule Inhibitors of Trypansoma cruzi Infection
    Leigh C Carmody, Andrew Germain, Douglas Barker, Cristina Galan-Rodriguez, Esther Bettiol, Ana Rodriguez, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: March 25, 2010; Last Update: February 10, 2011.
    • Probe Structure and Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
  • Identification of Modulators of the N370S Mutant Form of Glucocerebrosidase as a Potential Therapy for Gaucher Disease - Chemotype 2
    Omid Motabar, Wenwei Huang, Juan Jose Marugan, Noel Southall, Maria DeBernardi, Wei Zheng, and Ellen Sidransky.
    Received: March 24, 2010; Last Update: March 25, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Identification of Modulators of the N370S Mutant Form of Glucocerebrosidase as a Potential Therapy for Gaucher Disease - Chemotype 1
    Omid Motabar, Wenwei Huang, Juan Jose Marugan, Noel Southall, Maria DeBernardi, Wei Zheng, and Ellen Sidransky.
    Received: March 24, 2010; Last Update: May 5, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Identification of Small Molecule Antagonists of the Neuropeptide-S Receptor
    Samarjit Patnaik, Juan Marugan, Ke Liu, Wei Zheng, Annika Thorsell, Robert Eskay, Noel Southall, Markus Heilig, James Inglese, and Christopher Austin.
    Received: March 19, 2010; Last Update: December 16, 2010.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Toward Improved Therapy for Classic Galactosemia
    Matthew B Boxer, Min Shen, Cordelle Tanega, Manshu Tang, Kent Lai, and Douglas S Auld.
    Received: March 18, 2010; Last Update: March 3, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • Probe properties
    • 5 References
  • qHTS for Inhibitors of the Interaction of Thyroid Hormone Receptor and Steroid Receptor Coregulator 2
    Wenwei Huang, Ronald L Johnson, Ruili Huang, Jennifer Wichterman, Jong Yeon Hwang, and R Kip Guy.
    Received: March 18, 2010; Last Update: March 25, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Identification of a small molecule that selectively inhibits alpha-synuclein translational expression
    Nathan T Ross, Shailesh R Metkar, Hanh Le, Jason Burbank, Catherine Cahill, Andrew Germain, Lawrence MacPherson, Joshua Bittker, Michelle Palmer, Jack Rogers, and Stuart L Schreiber.
    Received: February 10, 2011; Last Update: February 15, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • 6 Appendices
  • Potent and selective inhibitors of NAD⁺-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD)
    Ajit Jadhav, Frank H Niesen, Lena Schultz, Udo Oppermann, David J Maloney, and Anton Simeonov.
    Received: March 4, 2010; Last Update: March 11, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • High Throughput Screening Assays for NOD1 Inhibitors - Probe 2
    Gavin Magnuson, Pasha Khan, Hongbin Yuan, Brock Brown, Daniela B Divlianska, Derek Stonich, Mahesh Peddibhotla, Ying Su, Shakeela Dad, Eduard Sergienko, Thomas DY Chung, Gregory P Roth, Carina Wimer, Paul Diaz, Ricardo G Correa, and John C Reed.
    Received: February 28, 2010; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 Bibliography
  • Selective GPR35 Antagonists - Probes 1 & 2
    Susanne Heynen-Genel, Russell Dahl, Shenghua Shi, Michelle Sauer, Santosh Hariharan, Eduard Sergienko, Shakeela Dad, Thomas DY Chung, Derek Stonich, Ying Su, Marc Caron, Pingwei Zhao, Mary E Abood, and Lawrence S Barak.
    Received: February 28, 2010; Last Update: October 4, 2010.
    • Probe(s) Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe(s)
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 References
  • A Cell Based Assay for the Identification of Lead Compounds with Anti-Viral Activity Against West Nile Virus
    DongHoon Chung, Robert Ardecky, Santhi Reddy Ganji, Nicholas DP Cosford, Colleen B Jonsson, Blake P Moore, Fuli Jia, Clinton Maddox, Sara N McKellip, E Lucile White, Subramaniam Ananthan, Shuang Feng, Lynn Rasmussen, Ying Su, Thomas DY Chung, Shakeela Dad, Nichole A Tower, and Marintha Heil.
    Received: February 27, 2010; Last Update: October 4, 2010.
    • Probe(s) Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe(s)
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 Bibliography
  • A Potent and Selective Inhibitor of Cdc42 GTPase
    Zurab Surviladze, Anna Waller, J Jacob Strouse, Cristian Bologa, Oleg Ursu, Virginia Salas, John F Parkinson, Genevieve K Phillips, Elsa Romero, Angela Wandinger-Ness, and Larry A Sklar; Chad Schroeder, Denise Simpson, Julica Nöth, Jenna Wang, Jennifer Golden, and Jeffrey Aubé.
    Received: February 27, 2010; Last Update: December 16, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe and prior art overview
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe Information and Characteristics
    • 4 Comparison to Prior Art for Cdc42 Inhibitors
    • 5 Bibliography
  • Selective KOP Receptor Antagonists: Probe 1
    Michael P Hedrick, Palak Gosalia, Kevin Frankowski, Shenghua Shi, Thomas E Prisinzano, Frank Schoenen, Jeffrey Aubé, Ying Su, S Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Partha Ghosh, Loribelle Milan, Susanne Heynen-Genel, Thomas DY Chung, Shakeela Dad, Marc Caron, Laura M Bohn, and Lawrence S Barak.
    Received: February 28, 2010; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 Bibliography
    • Appendix Synthetic procedures and compound characterization
  • Selective KOP Receptor Agonists: Probe 1 & Probe 2
    Michael P Hedrick, Palak Gosalia, Kevin Frankowski, Shenghua Shi, Thomas E Prisinzano, Frank Schoenen, Jeffrey Aubé, Ying Su, S Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Partha Ghosh, Loribelle Milan, Susanne Heynen-Genel, Thomas DY Chung, Shakeela Dad, Marc Caron, Laura M Bohn, and Lawrence S Barak.
    Received: February 28, 2010; Last Update: October 4, 2010.
    • Probe(s) Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe(s)
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 Bibliography
  • Discovery and development of the a highly selective M₁ Positive Allosteric Modulator (PAM)
    Thomas M Bridges, L Michelle Lewis, Eric S Dawson, C David Weaver, and Craig W Lindsley.
    Received: February 26, 2010; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
    • APPENDIX II Liquid Chromatography-Mass Spectrometry (LCMS) and Nuclear Magnetic Resonance (NMR) as prepared by Vanderbilt Specialized Chemistry Center
  • Probe Report for PME-1 Inhibitors
    DA Bachovchin, AE Speers, AM Zuhl, SJ Brown, BF Cravatt, Fernandez-Vega V, T Spicer, BA Mercer, J Ferguson, P Hodder, and HR Rosen.
    Received: February 26, 2010; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Probe Selection
    • Recommendations for the Scientific Use of This Probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 References
  • Identification of small molecules that selectively inhibit streptokinase expression without suppression of viability in Group A streptococci - Probe 3
    W Frank An, Shailesh R Metkar, Willmen Youngsaye, Partha P Nag, Cathy L Hartland, Douglas Barker, Jose R Perez, Hongmin Sun, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: February 26, 2010; Last Update: March 11, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and UPLC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • Identification of small molecules that selectively inhibit streptokinase expression without suppression of viability in Group A streptococci - Probe 2
    W Frank An, Shailesh R Metkar, Timothy A Lewis, Partha P Nag, Cathy L Hartland, Douglas Barker, Jose R Perez, Hongmin Sun, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: February 26, 2010; Last Update: March 11, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and LC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • A potent and selective small molecule Kir2.1 inhibitor
    Meng Wu, Hao-ran Wang, Haibo Yu, Elena Makhina, Jia Xu, Eric S Dawson, Corey R Hopkins, Craig W Lindsley, Owen B McManus, and Min Li.
    Received: February 26, 2010; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • A small molecule inhibitor of Caspase 1
    Matthew B Boxer, Min Shen, Douglas S Auld, James A Wells, and Craig J Thomas.
    Received: February 25, 2010; Last Update: March 3, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Probe Development Efforts to Identify Novel Antagonists of the Sphingosine 1-phosphate Receptor 4 (S1P4)
    M Oldstone, P Hodder, M Crisp, E Roberts, M Guerrero, M Urbano, S Velaparthi, J Zhao, H Rosen, MT Schaeffer, S Brown, and J Ferguson.
    Received: February 24, 2010; Last Update: December 16, 2010.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • High Throughput Screening Assays for NOD1 Inhibitors - Probe 1
    Gavin Magnuson, Pasha Khan, Hongbin Yuan, Brock Brown, Daniela B Divlianska, Derek Stonich, Mahesh Peddibhotla, Ying Su, Shakeela Dad, Eduard Sergienko, Thomas DY Chung, Gregory P Roth, Carina Wimer, Paul Diaz, Ricardo G Correa, and John C Reed.
    Received: January 23, 2010; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Comparative data showing probe specificity for target in biologically relevant assays
    • 5 Bibliography
  • Discovery of the first mAChR 5 (M5) selective ligand, an M5 Positive Allosteric Modulator (PAM)
    Thomas M Bridges, L Michelle Lewis, C David Weaver, and Craig W Lindsley.
    Received: December 18, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Screening Center Information: Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
    • APPENDIX II Liquid Chromatography-Mass Spectrometry (LCMS) and Nuclear Magnetic Resonance (NMR) as prepared by Vanderbilt Specialized Chemistry Center
  • Discovery of a potent, selective and in vivo active mGluR4 positive allosteric modulator
    Corey R Hopkins, Colleen M Niswender, L Michelle Lewis, C David Weaver, and Craig W Lindsley.
    Received: December 18, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Screening Center Information: Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
    • APPENDIX II Liquid Chromatography-Mass Spectrometry (LCMS) and Nuclear Magnetic Resonance (NMR) as prepared by Vanderbilt Specialized Chemistry Center
  • Selective Small Molecule Inhibitors of 12-Human Lipoxygenase (12-hLO)
    Ganesha Rai, Ajit Jadhav, Lena Schultz, Victor Kenyon, William Leister, Anton Simeonov, Theodore R Holman, and David J Maloney.
    Received: November 30, 2009; Last Update: March 25, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Identification of small molecules that selectively inhibit streptokinase expression without suppression of viability in Group A streptococci - Probe 1
    W Frank An, Shailesh R Metkar, Partha P Nag, Cathy L Hartland, Douglas Barker, Jose R Perez, Hongmin Sun, Lawrence MacPherson, Michelle Palmer, and Stuart L Schreiber.
    Received: November 16, 2009; Last Update: March 11, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
    • Appendix A Assay Summary Table
    • Appendix B Detailed Assay Protocols
    • Appendix C NMR and LC Data of Probe and Analogs
    • Appendix D Compounds Submitted to BioFocus
  • Campaign to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR)
    N Kumar, LA Solt, J Conkright, Y Wang, MA Istrate, SA Busby, RD Garcia-Ordonez, P Nuhant, T Burris, BA Mercer, P Hodder, WR Roush, H Rosen, and PR Griffin.
    Received: January 3, 2009; Last Update: March 11, 2011.
    • Probe Structure & Characteristics: ML124 & ML125
    • Recommendations for scientific use of the probe (ML124 and ML125)
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Campaign to Identify Agonists of Transient Receptor Potential Channels 3 and 2 (TRPML3 & TRPML2)
    SA Saldanha, C Grimm, BA Mercer, JY Choi, C Allais, WR Roush, S Heller, and P Hodder.
    Received: November 13, 2009; Last Update: May 5, 2011.
    • Recommendations for scientific use of the probe (ML118)
    • 1 Introduction
    • 3 Results
    • 4 Discussion
    • 5 References
  • HTS Assay for Discovery of Novel Metallo-Beta-lactamase (MBL) Inhibitors
    D Minond, SA Saldanha, T Spicer, Liu Qin, BA Mercer, WR Roush, and P Hodder.
    Received: November 13, 2009; Last Update: May 5, 2011.
    • Recommendations for scientific use of the probe (ML121)
    • 1 Introduction
    • 3 Results
    • 4 Discussion
    • 5 References
  • Selective HePTP Inhibitors: Probe 2
    Eduard Sergienko, Ekaterina Bobkova, Sharon Colayco, Justin Rascon, Xochella Chan, Stefan Vasile, Ying Su, Russell Dahl, Thomas DY Chung, Shakeela Dad, Tomas Mustelin, Wallace Liu, David A Critton, Rebecca Page, and Lutz Tautz.
    Received: November 1, 2009; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Selective HePTP Inhibitors: Probe 1
    Eduard Sergienko, Ekatarina Bobkova, Stefan Vasile, Hongbin Yuan Ying Su, Russell Dahl, Li Yang, Thomas DY Chung, Shakeela Dad, Tomas Mustelin, Wallace Liu, David A Critton, Rebecca Page, and Lutz Tautz.
    Received: November 1, 2009; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Small Molecule Inhibitors of Wee1 Degradation and Mitotic Entry
    F Madoux, J Mishra, BA Mercer, N Ayad, W Roush, P Hodder, and HR Rosen.
    Received: August 14, 2009; Last Update: March 25, 2011.
    • Recommendations for scientific use of the probe (ML118)
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Modulators of STAT Transcription Factors for the Targeted Therapy of Cancer (STAT3 Inhibitors)
    F Madoux, M Koenig, H Sessions, E Nelson, BA Mercer, M Cameron, W Roush, D Frank, and P Hodder.
    Received: August 28, 2009; Last Update: March 25, 2011.
    • Recommendations for scientific use of the probe (ML116)
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Modulators of STAT Transcription Factors for the Targeted Therapy of Cancer (STAT3 Activators)
    F Madoux, M Koenig, E Nelson, S Chowdhury, M Cameron, B Mercer, W Roush, D Frank, and P Hodder.
    Received: August 27, 2009; Last Update: December 16, 2010.
    • Probe Structure & Characteristics: ML115
    • Recommendations for scientific use of the probe (ML115)
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Probe Report for RBBP9 Inhibitors - Probe 2
    DA Bachovchin, AE Speers, SJ Brown, BF Cravatt, V Fernandez-Vega, T Spicer, BA Mercer, J Ferguson, P Hodder, and HR Rosen.
    Received: August 20, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics and Prior Art
    • Probe Selection
    • Recommendations for the Scientific Use of This Probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 References
  • Small-Molecule Inhibitors of Vaccinia-H1-Related Phosphatase VHR
    Lutz Tautz, Tomas Mustelin, Shuangding Wu, Sofie Vossius, Souad Rahmouni, Stefan Vasile, Eduard Sergienko, Derek Stonich, Hongbin Yuan, Ying Su, Russell Dahl, Yalda Mostofi, and Thomas DY Chung.
    Received: October 31, 2009; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Discovery of a small molecule inhibitor of ROMK with unprecedented selectivity
    Jerod S Denton, C David Weaver, Brian A Chauder, and Craig W Lindsley.
    Received: September 1, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
  • Discovery of a small molecule inhibitor of ROMK and Kir7.1
    Jerod S Denton, C David Weaver, L Michelle Lewis, Brian A Chauder, and Craig W Lindsley.
    Received: September 1, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
  • Identification of Potent and Selective Thyroid Stimulating Hormone Receptor Agonists
    Steve Titus, Wenwei Huang, Juan Marugan, Noel Southall, Jim Inglese, Christopher Austin, Wei Zheng, Erika Englund, Susanne Neumann, and Marvin Gershengorn.
    Received: September 1, 2009; Last Update: March 25, 2011.
    • Probe Structure & Characteristics
    • Recommendations for scientific use of the probe
    • 1 Introduction
    • 2 Materials and Methods
    • 3 Results
    • 4 Discussion
    • 5 References
  • Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM)
    L Michelle Lewis, Thomas M Bridges, Colleen M Niswender, C David Weaver, and Craig W Lindsley.
    Received: September 1, 2009; Last Update: October 20, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Bibliography
    • APPENDIX I Solubility, Stability and Reactivity data as determined by Absorption Systems
    • APPENDIX II Liquid Chromatography-Mass Spectrometry (LCMS) and Nuclear Magnetic Resonance (NMR) as prepared by Vanderbilt Specialized Chemistry Center
• Year 1 Reports
  • A high-throughput screen for pre-mRNA splicing modulators
    Douglas Auld, Min Shen, and Craig Thomas.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics: ML106
    • Recommendations for the scientific use of this probe
    • Probe Structure & Characteristics: ML105
    • Recommendations for the scientific use of this probe
    • The Role of Clk4 in alternate splicing
    • Assay Implementation and Screening
    • Probe Characterization: CID-3232621/ML106
    • Probe Characterization: CID-3234998/ML105
    • Bibliography
  • High throughput screening for SMA
    Steve Titus, Juan Marugan, Noel Southall, Jim Inglese, Chris Austin, and Wei Zheng; Elliot Androphy.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • High Throughput Screening for Small Molecule Inhibitors of Heparin-induced Tau Fibril Formation
    Ronald L Johnson, Wenwei Huang, and Ruili Huang; Alex Crowe, Carlo Ballatore, John Q Trojanowski, Kurt R Brunden, and Virginia M-Y Lee.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Probe Characterization
    • Synthesis of analogs
    • Appendices
    • Bibliography
  • HTS for Identification of Inhibitors against the ERK Signaling Pathway using a Homogenous Cell-based Assay
    Juan Marugan, Seameen Dehdashti, Wei Zheng, Noel Southall, James Inglese, and Christopher Austin.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Introduction
    • Materials and Methods
    • Results
    • Probe description
    • Bibliography
  • Antagonists of IAP-family anti-apoptotic proteins - Probe 1
    Kate Welsh, Hongbin Yuan, Derek Stonich, Ying Su, Xocella Garcia, Michael Cuddy, Richard Houghten, Eduard Sergienko, John C Reed, Robert Ardecky, Santhi Reddy Ganji, Marcos Lopez, Shakeela Dad, Thomas DY Chung, and Nicholas Cosford.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • uHTS for the identification of compounds that potentiate TRAIL-induced apoptosis of cancer cells
    Dmitri Rozanov, Brock Brown, Cheng-Tien Hung, Eduard Sergienko, Carlton Gasior, Palak Shah, Steve Vasile, Ying Su, Derek Stonich, Patrick Maloney, Greg Roth, Shakeela Dad, and Thomas DY Chung.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Three small molecule pan activator families of Ras-related GTPases
    Zurab Surviladze, Oleg Ursu, Fabiola Miscioscia, Ramona Curpan, Liliana Halip, Cristian Bologa, Tudor Oprea, Anna Waller, Juan Strouse, Virginia Salas, Yang Wu, Bruce Edwards, Angela Wandinger-Ness, and Larry Sklar.
    Received: May 18, 2009; Last Update: September 2, 2010.
    • Probe (1) Structure & Characteristics
    • Probe (2) Structure & Characteristics
    • Probe (3) Structure & Characteristics
    • Summary of Recommended Usage and State of the Art of G Protein Activators
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probes
    • 4 Appendices
    • 5 Bibliography
  • Therapeutic Inhibitors of Phosphomannose Isomerase - Probe 2
    Michael Hedrick, Brock Brown, Justin Rascon, Eduard Sergienko, Vandana Sharma, Bobby Ng, Mie Ichikawa, Hudson Freeze, Derek Stonich, Ying Su, Shakeela Dad, Thomas DY Chung, Russell Dahl, and Nick Cosford.
    Received: May 17, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 2
    Marion Lanier, John Cashman, Eduard Sergienko, Xochella Garcia, Brock Brown, Justin Rascon, Sonoko Narisawa, Ana Maria Simao, José Luis Millán, Derek Stonich, Ying Su, Russell Dahl, and Thomas DY Chung.
    Received: May 16, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Bibliography
  • Probe Report for NOX1 Inhibitors
    SJ Brown, D Gianni, G Bokoch, BA Mercer, P Hodder, and HR Rosen.
    Received: April 23, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Therapeutic Inhibitors of Phosphomannose Isomerase - Probe 1
    Michael Hedrick, Brock Brown, Justin Rascon, Eduard Sergienko, Vandana Sharma, Bobby Ng, Mie Ichikawa, Hudson Freeze, Derek Stonich, Ying Su, Thomas DY Chung, Russell Dahl, and Nick Cosford.
    Received: April 21, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • HTS identification of compounds activating TNAP at an intermediate concentration of phosphate acceptor detected in luminescent assay
    Xochella Chan, Brock Brown, Michael Hedrick, Justin Rascon, José Luis Millán, Eduard Sergienko, Greg Roth, Santhi Reddy, Shakeela Dad, Thomas DY Chung, Nicholas Cosford, Derek Stonich, and Ying Su.
    Received: April 21, 2009; Last Update: September 2, 2010.
    • Probes Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • The Role of PHOSPHO1 in the Initiation of Skeletal Calcification
    Dereck Stonich, Ying Su, Shakeela Dad, Santhi Reddy, Yalda Mostofi, Dahl Russell, Thomas DY Chung, Nicholas Michael Hedrick, Justin Rascon, Xochella Garcia, Eduard Sergienko, José Luis Millán, Derek Stonich, and Nicholas Cosford.
    Received: April 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Placental Alkaline Phosphatase (PLAP) Luminescent HTS assay - Probe 1
    Eduard Sergienko, Xochella Garcia, Brock Brown, Justin Rascon, Sonoko Narisawa, Ana Maria Simao, José Luis Millán, Derek Stonich, Ying Su, Pasha Khan, Greg Roth, Layton Smith, Shakeela Dad, Thomas DY Chung, and Nicholas DP Cosford.
    Received: April 18, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Identification of lipid storage modulators
    Mathias Beller, Craig Thomas, Min Shen, and Douglas Auld.
    Received: April 16, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • Assay Implementation and Screening
    • Probe Characterization
    • Probe
    • Compound preparation
    • Bibliography
  • Identification of activators for the M2 isoform of human pyruvate kinase
    Douglas Auld, Min Shen, Amanda P Skoumbourdis, Jian-kang Jiang, Matthew Boxer, Noel Southall, James Inglese, and Craig Thomas.
    Received: April 16, 2009; Last Update: August 6, 2010.
    • Probe Structure and Characteristics
    • Recommendations for the scientific use of these probes
    • Assay Implementation and Screening
    • Known probe properties
    • Bibliography
  • Probe Report for RBBP9 Inhibitors - Probe 1
    SJ Brown, DA Bachovchin, BF Cravatt, V Fernandez-Vega, T Spicer, BA Mercer, P Hodder, and HR Rosen.
    Received: March 13, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Probe Report for P97/cdc48 Inhibitors
    SJ Brown, T-F Chou, R Deshaies, E Roberts, M Guerrero, D Minond, BA Mercer, P Hodder, and HR Rosen.
    Received: March 6, 2009; Last Update: August 6, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Identification of Functionally Selective Small Molecule Antagonists of the Neuropeptide-S Receptor: Naphthopyranopyrimidines
    Juan Marugan, Ke Liu, Wei Zheng, Robert Eskay, Noel Southall, Markus Heilig, James Inglese, and Christopher Austin.
    Received: February 13, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Discovery of a Highly Selective KCC2 Antagonist
    Craig Lindsley, Michelle Lewis, Dave Weaver, and Eric Delpire.
    Received: February 1, 2009; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • PubChem Primary Assay Description
    • Bibliography
  • Inhibitors of Protein Folding: DnaK
    J Cellitti, Z Zhang, S Wang, B Wu, D Guiney, and M Pellecchia.
    Received: January 15, 2009; Last Update: September 2, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
  • Probe Report for NPY-Y2 Receptor Antagonists
    SA Saldanha, SP Brothers, T Spicer, M Cameron, BA Mercer, P Chase, P McDonald, C Wahlestedt, and PS Hodder.
    Received: January 13, 2009; Last Update: August 6, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • 1 Scientific Rationale for Project
    • 2 Project Description
    • 3 Probe
    • 4 Appendices
    • 5 Bibliography
    • Brain Penetrance Data
  • Discovery of a Highly Selective in vitro and in vivo M1 Allosteric Agonist Probe
    Craig Lindsley, Michelle Lewis, and Dave Weaver.
    Received: December 3, 2008; Last Update: October 4, 2010.
    • Probe Structure & Characteristics
    • Recommendations for the scientific use of this probe
    • PubChem Primary Assay Description
    • Probe Chemical Lead Optimization Strategy
    • Bibliography