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Precon


	Conference Proceeding CD Now Available Single Copy - $750.00Site License - $1,995.00	Speaker Presentations Poster Abstracts and More!

FDT

SUNDAY, APRIL 27

2:05 Chairperson’s Introduction
David Bailey, Ph.D, Chief Executive Officer, IOTA Pharmaceuticals Ltd

2:15 Fragment Library Design: Maximizing Success through Intelligent Selection
Douglas R. Davies, Ph.D., Sr. Research Scientist, Crystallography, deCODE biostructures, Inc.

Fragment properties and the “Rule of 3”
Privileged scaffolds and fragment selection
Chemical “handles”: a benefit or a burden?
Ligand efficiency and “Fragments of Life”
Pooling compounds for diversity

2:45 Fragment Library Screening: Exploring Pharma Space with Larger Fragment Libraries
David Bailey, Ph.D, Chief Executive Officer, IOTA Pharmaceuticals Ltd

Measuring diversity within fragment libraries
Building fragment libraries for specialised screening applications
IOTA and Vitas-M Lab 5000-component, Diverse and Medchem Fragment libraries
Validating fragment selection in practice: Case Studies with GPCRs

3:15 High-throughput Crystallography in Context: Efficiency through Miniaturisation
Stefan Steinbacher, Project Manager, Proteros biostructures GmbH

High-throughput crystallography to translate fragments into leads
Overview of published results and applications of the technology
Proteros’s crystallization technology
Case studies with pharmaceutical targets

3:45 SPR: From Fragment Screening to Lead Optimization - the Biacore Experience
Per Källblad Ph.D., Chief Executive Officer, Beactica AB

Surface plasmon resonance (SPR) as a tool for fragment-based drug discovery
Technology benefits and technical challenges
Case studies: MMP, HIV and HCV drug discovery

4:15 SPR: From fragment screening to Lead Optimization - the Graffinity Experience
Thomas Neumann, Head of Screening, Graffinity Pharmaceuticals GmbH

The principles of array-based fragment screening
Advantages and applications of Graffinity’s fragment-screening approach
Selectivity and binding mode studies at a primary screening level
Case studies with pharmaceutical targets

4:45 Session Wrap-up