| SUNDAY |
| 2:00 pm - 11:00 pm | Arrival and Check-in |
| 6:00 pm | Dinner |
| 7:30 pm - 7:40 pm | Welcome / Introductory Comments by GRC Site Staff |
| 7:40 pm - 9:30 pm | New Technologies and Drug Discovery |
| Discussion Leader: Daryl Sauer (Abbott Labs) |
| 7:40 pm - 8:00 pm | Tom Beattie (TRB Associates)
"Combinatorial Chemistry: Past, Present and Future" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Anabella Villalobos (Pfizer)
"Chemical Efficiencies and Changing the Way We do Medicinal Chemistry" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Jim Summers (Abbott Labs)
"Meeting the Challenges of the Pharmaceutical Industry - The Role of Technology in a Winning R&D Strategy" |
| 9:20 pm - 9:30 pm | Discussion |
| MONDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Organic / Bio-organic Chemistry |
| Discussion Leader: Oliver Kappe (Karl-Franzens University) |
| 9:00 am - 9:45 am | Stephen Martin (University of Texas-Austin)
"Aspects of Protein-Ligand Interactions: What are the Energetic Consequences of Ligand Preorganization?" |
| 9:45 am - 9:55 am | Discussion |
| 9:55 am | Coffee Break / Group Photo |
| 10:30 am - 11:00 am | Bruce Lipshutz (University of California-Santa Barbara)
"Enabling Technologies Based on the Chemistry of Coenzyme Q10" |
| 11:00 am - 11:10 am | Discussion |
| 11:10 am - 11:40 am | Valery Fokin (Scripps Research Institute)
"Catalytic Dipolar Cycloadditions: Diversity and Function" |
| 11:40 am - 11:50 am | Discussion |
| 11:50 am - 12:20 pm | Ohyun Kwon (UCLA)
"Phosphine Catalysis of Allenes in Diversity-Oriented Synthesis" |
| 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 | Enabling Technologies in Drug Discovery |
| Discussion Leader: Tom Sowin (Abbott Labs) |
| 7:30 pm - 8:00 pm | Andrew Combs (Incyte)
"A Pragmatic Approach to Increasing Productivity in Discovery Chemistry" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Craig Lindsley (Vanderbilt University)
"Preclinical Drug Discovery in an Academic Setting - It is Possible" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Steve Haswell (University of Hull)
"Intelligent Drug Design Through the Application of Micro Fluidic Technology" |
| 9:20 pm - 9:30 pm | Discussion |
| TUESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Structural Approaches and Drug Design |
| Discussion Leader: Philip Hajduk (Abbott Labs) |
| 9:00 am - 9:35 am | Marc Jacobs (Vertex Pharmaceuticals)
"Leveraging X-ray Structural Information in Gene-family Based Drug Discovery: Protein Kinases" |
| 9:35 am - 9:45 am | Discussion |
| 9:45 am - 10:20 am | Rod Hubbard (Vernalis)
"Experiences in fragment-based discovery" |
| 10:20 am - 10:30 am | Discussion |
| 10:30 am | Coffee Break |
| 11:00 am - 11:35 am | Philip Hajduk (Abbott Labs)
"A Statistical Analysis of Chemical Substituents Utilized in Lead Optimization" |
| 11:35 am - 11:45 am | Discussion |
| 11:45 am - 12:20 pm | Maurizio Pellecchia (Burnham Institute)
"Structure and NMR-Based Approaches to Protein Kinase Inhibition" |
| 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 | Medicinal Chemistry Case Studies |
| Discussion Leader: Craig Lindsley (Vanderbilt) |
| 7:30 pm - 8:00 pm | Scott Wolkenberg (Merck)
"Selective Agonists of Somatostatin Receptor Subtype 2 (sstr2): Application of an Iterative Analogue Library Approach" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Alice Rodriguez (Vanderbilt)
"From HTS to lead optimization using technology enabled synthesis: Development of novel allosteric potentiators of mGluR5" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Joe Salvino (Cephalon)
"Practical Approaches Toward Lead Finding and Lead Optimization Library Synthesis" |
| 9:20 pm - 9:30 pm | Discussion |
| WEDNESDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am - 12:30 pm | Libraries for Chemical Biology |
| Discussion Leader: Kip Guy (St. Jude) |
| 9:00 am - 9:35 am | Ben Cravatt (Scripps Research Institute)
"Mapping enzyme active sites in complex proteomes" |
| 9:35 am - 9:45 am | Discussion |
| 9:45 am - 10:20 am | Doron Greenbaum (University of Pennsylvania)
"A Chemical Biology Approach to Understand Protease Function in the Malarial Parasite" |
| 10:20 am - 10:30 am | Discussion |
| 10:30 am | Coffee Break |
| 11:00 am - 11:35 am | Jack Taunton (UCSF)
"New Chemical Tools for Exploring the Kinomes of People and Parasites" |
| 11:35 am - 11:45 am | Discussion |
| 11:45 am - 12:20 pm | Jeremy Mallari (St. Jude)
"Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB" |
| 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 |
| 7:00 pm - 7:30 pm | Business Meeting |
| (Nominations for the next Vice Chair; Discuss future Site & Scheduling preferences; Discuss Conference Name Change) |
| 7:30 pm - 9:30 pm | NIH CMLD Projects |
| Discussion Leader: Jeff Aube (University of Kansas) |
| 7:30 pm - 7:55 pm | James Panek (Boston University)
"Expanding stereochemical and skeletal diversity using chiral organosilanes" |
| 7:55 pm - 8:00 pm | Discussion |
| 8:00 pm - 8:25 pm | Jeff Aube (University of Kansas)
"Application of Domino Reactions to Library Synthesis" |
| 8:25 pm - 8:30 pm | Discussion |
| 8:30 pm - 8:55 pm | Jared Shaw (Broad Institute of Harvard and MIT)
"New strategies for high throughput synthesis and target identification" |
| 8:55 pm - 9:00 pm | Discussion |
| 9:00 pm - 9:25 pm | Peter Wipf (University of Pittsburgh)
"Parallel Synthesis of Heterocycles - Something Old, Something New, Something Borrowed, Something Blue" |
| 9:25 pm - 9:30 pm | Discussion |
| THURSDAY |
| 7:30 am - 8:30 am | Breakfast |
| 8:30 am - 9:00 am | Business Meeting |
| (Vice Chair Candidate Presentations) |
| 9:00 am - 12:30 pm | Academic Combichem / Library Generation |
| Discussion Leader: Jared Shaw (Broad Institute of Harvard and MIT) |
| 9:00 am - 9:35 am | Ian Baxendale (Cambridge University)
"Multi-step flow synthesis: Training to be a plumber" |
| 9:35 am - 9:45 am | Discussion |
| 9:45 am - 10:20 am | Sergey Kozmin (University of Chicago)
"From Practical High-Throughput Synthesis of Pure Small-Molecule Libraries to Discovery of New Cell-Modulators" |
| 10:20 am - 10:30 am | Discussion |
| 10:30 am | Coffee Break |
| 11:00 am - 11:35 am | Dave Bergbreiter (Texas A&M University)
"Separation Strategies for Synthesis and Catalysis that Use Soluble Polymers" |
| 11:35 am - 11:45 am | Discussion |
| 11:45 am - 12:20 pm | Nikki Pohl (Iowa State University)
"Automated Solution-phase Iterative Oligosaccharide Synthesis" |
| 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 |
| 7:00 pm - 7:30 pm | Business Meeting |
| (Fill out Conference Evaluation Forms; Election of the next Vice Chair) |
| 7:30 pm - 9:30 pm | Medicinal Chemistry Case Studies |
| Discussion Leader: Joe Salvino (Cephalon) |
| 7:30 pm - 8:00 pm | James Leahy (Exelixis Pharmaceuticals)
"High Throughput Methodology in Kinase Inhibitors" |
| 8:00 pm - 8:10 pm | Discussion |
| 8:10 pm - 8:40 pm | Chris Sarko (Boehringer-Ingelheim)
"Hit to Lead Evaluation of Benzimidazole Inhibitors of ITK: From General Screening Library to Lead Series" |
| 8:40 pm - 8:50 pm | Discussion |
| 8:50 pm - 9:20 pm | Roland Dolle (Aldolor)
"New Reagents for N-Heterocyclization of Primary Amines" |
| 9:20 pm - 9:30 pm | Discussion |
| FRIDAY |
| 7:30 am - 8:30 am | Breakfast |
| 9:00 am | Depart |
