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Part I. Overviews: 1. Harnessing the power of chemistry for biology and medicine Cheryl L. Meyerkord and Haian Fu; 2. Chemical genomics: exploring biology with small organic molecules Nicholas Aberle and Craig M. Crews; 3. Chemical proteomics Akihisa Matsuyama, Yoko Yashiroda and Minoru Yoshida; Part II. Molecules for Chemical Genomics: 4. Diversity-oriented synthesis Warren R. J. D. Galloway, Richard J. Spandl, Andreas Bender, Gemma L. Thomas, Monica Diaz-Gavilan, Kieron M. G. O’Connell and David R. Spring; 5. Targeted chemical libraries Gregory P. Tochtrop and Ryan E. Looper; 6. Fragment-based ligand discovery Sandra Bartoli, Antonella Squarcia and Daniela Fattori; 7. Basics and principles for building natural product-based libraries for HTS Ronald J. Quinn; Part III. Basics of High Throughput Screening: 8. Essentials for high throughput screening operations Stewart P. Rudnicki, James V. Follen, Nicola J. Tolliday and Caroline E. Shamu; 9. High content analysis and screening: basics, instrumentation and applications Paul A. Johnston; 10. Phenotypic screens with model organisms Grant N. Wheeler, Robert A. Field and Matthew L. Tomlinson; 11. Screening informatics and ChemInformatics Lestyn Lewis; Part IV. Chemical Genomics Assays and Screens: 12. Basics on HTS assay design and optimization Eduard Sergienko; 13. Molecular sensors for transcriptional and post-transcriptional assays Douglas S. Auld and Natasha Thorne; 14. Fluorescence-based platforms for HTS assays – FP and TR-FRET Yuhong Du and Jonathan Havel; 15. Compound profiling with high content screening methodology Thomas Mayer and Stephan Schürer; 16. Use of transgenic zebrafish in a phenotypic screen for angiogenesis inhibitors Jaeki Min, Yuhong Du, Brenda Bondesen, Brian Revennaugh, Peter Eimon and Ray Dingledine; 17. Flow cytometry multiplexed screening methodologies Virginia M. Salas, J. Jacob Strouse, Zurab Surviladze, Irena Ivnitski-Steele, Bruce S. Edwards and Larry A. Sklar; 18. Basic principles and practices of computer-aided screening and drug design Chao-Yie Yang, Denzil Bernard and Shaomeng Wang; 19. Computational approach for drug target identification Honglin Li, Mingyue Zheng, Xiaofeng Liu and Hualiang Jiang; 20. Label-free biosensor technologies for assay development and HTS Yuhong Du and Arron Xu; Part V. Chemical Genomics and Medicine: 21. Pharmacogenomics to link genetic background with therapeutic efficacy and safety Mark M. Bouzyk, Weining Tang and Brian Leyland-Jones; 22. Drugs, genomic response signatures, and customized cancer therapy Rafael Rosell, Teresa Moran and Miguel Taron; Appendix. Current drug targets and the druggable genome Andreas Russ.

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