| SUNDAY |
| 2:00 pm - 9:00 pm | Arrival and Check-in |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | TARGET CLASS LIBRARIES |
| Discussion Leader: Christine Brotherton-Pleiss (Roche Biosciences) |
| 7:30 pm - 7:50 pm | Conference Overview and Introductions (Sam Gerritz and Site Coordinator) |
| 7:50 pm - 8:10 pm | Hartmuth Kolb (UCLA)
"In Situ Click Chemistry: Enzyme Inhibitors Made to Their Own Specifications" |
| 8:10 pm - 8:20 pm | Discussion |
| 8:20 pm - 8:50 pm | David Drewry (GlaxoSmithKline)
"Heterocyclic Chemistry in Kinome Drug Discovery" |
| 8:50 pm - 9:00 pm | Discussion |
| 9:00 pm - 9:30 pm | Jon Ellman (UC-Berkeley)
"Combinatorial Chemistry Applied to the Efficient and Systematic Study of Proteases" |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:30 am | Group Photo |
| 9:00 am - 12:30 pm | CASE STUDIES 1 |
| Discussion Leader: Daryl Sauer (Abbott) |
| 9:00 am - 9:30 am | Brian McKittrick (Schering-Plough)
"From Solid Phase Synthesis of Large Mixtures to Solution Phase Synthesis of Discrete Compound Libraries: A Brief History of High-Throughput Chemistry at SPRI " |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Rachael Hunter (Pharmacopeia)
"MCH: A Novel Pharmaceutical Target For The Treatment Of Obesity" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Guy Breitenbucher (Johnson & Johnson)
"Determination of Additivity in Combinatorial Libraries and its Implications in the Interpretation of SAR: A CCK-1 antagonist case study" |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 12:00 pm | Craig Lindsley (Merck)
"Lead Optimization Driven by Iterative Analogue Library Synthesis: Development of Novel Allosteric Akt Kinase Inhibitors" |
| 12:00 pm - 12:10 pm | Discussion |
| 12:10 pm - 12:30 pm | Brett Bookser (Metabasis Therapeutics)
"High Throughput 5-Minute Microwave Synthesis of Nucleosides" |
| 12:30 pm | Lunch |
| 1:30 pm - 4:00 pm | Free Time |
| 4:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | LIBRARY SYNTHESIS CAPACITY: RENT OR BUY? |
| Discussion Leader: John Porco (Boston University) |
| 7:30 pm - 8:00 pm | Libing Yu (ArQule Inc.)
"Built for rent: case study on ArQule's HT chemistry support for pharmaceutical/biotech collaborators" |
| 8:00 pm - 8:30 pm | Bill Coates (GlaxoSmithKline)
"Rent or Buy? The best of both worlds, and then some...." |
| 8:30 pm - 9:00 pm | Combined Discussion |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | LIBRARIES BASED ON NATURAL PRODUCTS |
| Discussion Leader: David Oare (Gilead) |
| 9:00 am - 9:30 am | Takashi Takahashi (Tokyo Institute of Technology)
"Solid- and Solution-Phase Syntheses Toward the Library of Natural Products" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Gunda Georg (University of Kansas)
"Synthesis of Nitrogen-Containing, Natural Product-Inspired Combinatorial Libraries" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Ganesan (University of Southampton)
"Natural Products, Metals and Drug Discovery" |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 11:50 am | Annaliese Franz (Harvard University)
"Natural Product-Inspired Libraries with Unnatural Motifs: Synthesis and Biological Evaluation of Diverse Silyl-Functionalized Compounds" |
| 11:50 am - 12:00 pm | Discussion |
| 12:00 pm - 12:20 pm | Scott Schaus (Boston University)
"Asymmetric Catalytic Methods to Library Design and Synthesis: The Direct Mannich Reaction of b-Keto Esters with Acyl Imines" |
| 12:20 pm - 12:30 pm | Discussion |
| 12:30 pm | Lunch |
| 1:30 pm - 4:00 pm | Free Time |
| 4:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | AN OVERVIEW OF THE CENTERS FOR CHEMICAL METHODOLOGY AND LIBRARY DEVELOPMENT (CMLD) |
| Discussion Leader: John Schwab (NIH/NIGMS) |
| 7:30 pm - 7:40 pm | CMLD Overview by John Schwab |
| 7:40 pm - 8:00 pm | John Porco (Boston University CMLD)
"Expanded Diversity Using Stereocontrolled Synthesis: Recent Progress of the CMLD-BU" |
| 8:00 pm - 8:20 pm | Stefan Werner (University of Pittsburgh CMLD)
"From Chemical Methodologies to Library Development: Design, Synthesis and Biological Evaluation of Discovery and Focused Libraries in the UPCMLD" |
| 8:20 pm - 8:40 pm | Jeff Aube (University of Kansas CMLD)
"Snapshots from the KU-CMLD" |
| 8:40 pm - 9:00 pm | Jared Shaw (Harvard University CMLD)
"Integrated Approaches to Methodology Discovery and Library Development" |
| 9:00 pm - 9:30 pm | Combined Discussion |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | SYNTHESIS AND SCREENING OF BIOPOLYMERS |
| Discussion Leader: Shelli McAlpine (San Diego State University) |
| 9:00 am - 9:30 am | Peter Seeberger (ETH)
"Automated Oligosaccharide Synthesis and Carbohydrate Arrays: A Versatile Platform for Biological Research and Drug Discovery" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Laura Kiessling (University of Wisconsin- Madison)
"Combinatorial Chemistry for Chemical Glycobiology" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:10 am | Alice Ting (M.I.T.)
"Library-based Approach to Development of Small-Molecule and Genetically-Encoded Reporters for Cell Signaling" |
| 11:10 am - 11:20 am | Discussion |
| 11:20 am - 11:40 am | Aaron Beeler (Boston University CMLD)
"The Synthesis of Complex Macrodiolides Through Cyclodimerization of Polypropionate-Like Hydroxy Ethers" |
| 11:50 am - 12:00 pm | Discussion |
| 12:00 pm - 12:30 pm | Hiro Suga (University of Tokyo)
"Discovery of RNA catalysts using Artificial Evolution and its Infinite Potential" |
| 12:30 pm | Lunch |
| 1:30 pm - 4:00 pm | Free Time |
| 4:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | DISCOVERY OF NEW REACTIONS |
| Discussion Leader: John Quinn (Albany Molecular) |
| 7:30 pm - 7:50 pm | Rolf Breinbauer (University of Dortmund)
"Electrons as a Reagent in Solid-Phase Organic Synthesis" |
| 7:50 pm - 8:00 pm | Discussion |
| 8:00 pm - 8:30 pm | Scott Gilbertson (University of Texas Medical Branch)
"Parallel Approaches to Phosphine and NHC Ligands" |
| 8:30 pm - 8:40 pm | Discussion |
| 8:40 pm - 9:10 pm | Eric Jacobsen (Harvard University)
"Seeking General Yet Selective Asymmetric Catalysts" |
| 9:10 pm - 9:20 pm | Discussion |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | CASE STUDIES 2 |
| Discussion Leader: Michael Lawrence (Bristol-Myers Squibb) |
| 9:00 am - 9:30 am | Jeremy Green (Vertex)
"Application of Parallel Solution- and Solid-Phase Synthetic Methods in Conjunction with Structure-Based Design in MAP Kinase Inhibitor Discovery" |
| 9:30 am - 9:40 am | Discussion |
| 9:40 am - 10:10 am | Alexandr Kiselyov (ChemDiv)
"Targeting Hh Signaling Transduction Pathway with Small Molecules" |
| 10:10 am - 10:20 am | Discussion |
| 10:20 am - 10:50 am | Coffee Break |
| 10:50 am - 11:20 am | Christopher Hulme (Eli Lilly) |
| 11:20 am - 11:30 am | Discussion |
| 11:30 am - 12:00 pm | Ivan Lorkovic (Gas Reaction Technologies, Inc.)
"Rapid Evaluation of Metal Oxide/Metal Bromide Solid Mediators in Alkane Partial Oxidation Chemistry" |
| 12:00 pm - 12:10 pm | Discussion |
| 12:10 pm - 12:30 pm | Business Meeting |
| 12:30 pm | Lunch |
| 1:30 pm - 4:00 pm | Free Time |
| 4:00 pm - 6:00 pm | Poster Session |
| 6:00 pm | Dinner |
| 7:30 pm - 9:30 pm | CHEMICAL GENETICS |
| Discussion Leader: R. Kip Guy (University of California- San Francisco) |
| 7:30 pm - 7:50 pm | Akira Kawamura (CUNY-Hunter College)
"Photoactive Molecular Baits for Protein Fishing" |
| 7:50 pm - 8:00 pm | Discussion |
| 8:00 pm - 8:30 pm | Young-Tae Chang (New York University)
"Facilitated Chemical Genetics using Tagged Small Molecule Library" |
| 8:30 pm - 8:40 pm | Discussion |
| 8:40 pm - 9:10 pm | Tom Kodadek (University of Texas-Southwestern Medical Center)
"Functional and Analytical Applications of Combinatorial Peptoid Libraries In Biology and Medicine" |
| 9:10 pm - 9:20 pm | Discussion |
| FRIDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am | Depart |
