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Please contact FBLD 2010 Administrator for password details.
Sunday, 10th October, Noon - Registration opens
13:00 - 14:30 | CCG Workshop "Free MOE Workshop" |
14:30 - 15:30 | CCG + BioSolveIT "Synergies for FBLD" |
15.30 - 17:00 | BioSolveIT Workshop "Fragment-Based Ligand Design in Teams" |
17:30 - 19:00 | Mixer with food and drink |
Monday 11th October:
Fragment Libraries and Chemical Space
(Andrew Leach & Mike Hann, GlaxoSmithKline, co-chairs)
8:00 - 8:45 | Plenary Introduction: "Current Perspectives in Fragment-Based Discovery" Rod Hubbard, Vernalis & University of York |
8:45 - 9:25 | “Enumeration, Mapping and Scoring of Chemical Space”, Jean-Louis Reymond, University of Berne |
9:25 - 9:55 | “From Druggability, to Ligand Efficiency, to the Universe of Heterocyclic Rings”, Colin Groom, Cambridge Crystallographic Data Centre |
9:55 - 10:25 | Coffee & Tea |
10:25 - 10:55 | “Design and Application of LEF, a Library of Chemical Fragments with Different Local Environment of Fluorine”, Anna Vulpetti, Novartis |
10:55 - 11:25 | “Shape Diversity in Fragment Library Design: Theory and Practice”, Ken Brameld, Roche |
11:25 - 11:55 | "Fragment Based Druggability Screening to Predict Lead Discovery Success", Fredrik Edfeldt, AstraZeneca R&D |
11:55 - 12:25 | Three - Four 10 minute poster/vendor talks to be selected in August 2010 |
12:30 - 13:30 | Lunch, Posters & Vendors |
Biophysics A: Hit Identification
(Don Huddler. GlaxoSmithKline, Chair)
13:30 - 14:10 | “NMR and Computational Approaches to Fragment Hit ID” Maurizio Pellecchia, Burnham Institute for Medical Research |
14:10 - 14:40 | “Ligand-Observed NMR Fragment Screening”, Ben Davis, Vernalis |
14:40 - 15:10 | “Fragment Library Screening with SPR”, Tony Giannetti, Genentech |
15:10 - 15:40 | “Automated SPR Data Processing and Sensogram Classification”, Constantine Kreatsoulas, Merck |
15:40 - 16:10 | Coffee & Tea |
16:10 - 16:40 | “Biophysical Ligand Screening of Soluble and Membrane-Bound Targets”, Gregg Siegal, ZoBio & Universiteit Leiden |
16:40 - 17:10 | "Small Molecule Fragment Screening with Biolayer Interferometry on the ForteBio Octet Red Instruments", Charles A. Wartchow, Hoffman La Roche |
18:00 - | Food, Drink, Posters & Vendors |
Tuesday 12th October:
Biophysics B: Screening and Characterization Technologies
(Tony Giannetti, Genentech, Chair)
8:30 - 9:15 | “Overview of Biophysics for Fragment Discovery and Characterization”, Glynn Williams, Astex Therapeutics |
9:15 - 9:45 | “Fragment Screening against Membrane Receptors using SPR - Seriously?”, Rebecca Rich, University of Utah |
9:45 - 10:15 | “Comparison of plate-based biophysical binding assay methods for fragment library screening”, Kartik Narayan, Merck |
10:15 - 10:45 | Coffee & Tea |
10:45 - 11:15 | “Predicting success from X-ray Cystallographic Screening of Fragments”, Doug Davies, Emerald BioStructures |
11:15 - 11:45 | “Culling Through Fragment Hits with Biophysical Approaches”, Bill Metzler, Bristol-Myers Squibb |
11:45 - 12:15 | "Fragment-based screening for inhibitors of PDE4A using enthalpy arrays and X-ray crystallography", Michael Recht, Palo Alto Research Centre |
12:15 - 13:45 | Lunch, Posters & Exhibitors |
Chemistry Follow-up Strategies
(Dan Erlanson, Carmot Therapeutics, Chair)
13:30 - 14:00 | “From Weak NMR-Detected Fragment Hits to First-in-class Recommendation Candidates for BACE-1”, Dan Wyss, Merck |
14:00 - 14:30 | "Ups and downs of structurally un-enabled fragment optimization", Adam Renslo, University of California, San Francisco |
14:30 - 15:00 | “Targeting Protein-Protein Interactions via Kinetic Target-Guided Synthesis“, Roman Manetsch, University of South Florida |
15:00 - 15:30 | Coffee & Tea |
15:30 - 16:00 | “Shortening the Time to a Successful Fragment HTL Campaign”, Sandy Farmer, Boehringer Ingelheim Pharmaceuticals, Inc |
16:00 - 16:30 | "Discovery of new high-affinity PDE10 inhibitors using fragment based lead generation and knowledge-based design", Jeffrey S. Albert, AstraZeneca |
16:30 - 16:50 | "Novel PDK1 Inhibitors Discovered through FBLD", M. Catherine Johnson, Pfizer |
16:50 - 17:10 | "FBLD: A PDK1 Case Study", Jeffrey M. Axten, GlaxoSmithKline |
18:00 - | Conference Banquet |
Wednesday 13th:
Success Stories and Chemical Biology
(Rod Hubbard, Vernalis & The University of York, Chair)
8:30 - 9:10 | “Fragment-Based Ligand Discovery : New Opportunities with Well-Known Targets”, Wolfgang Jahnke, Novartis |
9:10 - 9:50 | “Targeting the Intractable”, Chaohong Sun, Abbott Labs |
9:50 - 10:30 | “Beyond Growing and Linking: Impact of Fragments on the Discovery of Kinase Inhibitors”, Andreas Kuglstatter, Roche |
10:30 - 11:00 | Coffee & Tea |
11:00 - 11:30 | "Fragment based drug discovery of selective inhibitors of Fibroblast Growth Factor Receptor (FGFr)", Gordon Saxty, Astex Therapeutics |
11:30 - 12:15 | “Fragments - a Story That Will Run and Run”. Chris Abell, University of Cambridge |
12:30 - | Close of Conference |
Click to download Conference Flyer (PDF) or Conference Agenda (PDF).