Fragment-based Lead Discovery Conference 2008
San Diego, CA February 18-20

FBLD Resources

Implementation of Fragment-based Lead Discovery depends on high quality, specialized products and services. The Exhibitors and Sponsors of FBLD 2008 represent the best companies to find products, services, and collaborations for FBLD Research. Below, please find a list of the FBLD Resources available from FBLD 2008 Exhibitors and Sponsors, and check back soon for updates on their planned activities for the conference.

FBLD 2008 Exhibitor/Sponsor Resources

Sponsor	Company Description Accelrys develops and commercializes Scientific Business Intelligence software for the integration, mining, analysis, modeling and simulation, management and interactive reporting of scientific data. Our solutions are used by biologists, chemists, materials scientists, and information technology professionals for product design as well as drug discovery and development. Our technology and services are designed to meet the needs of today's leading research and development organizations.
Premier Sponsor/Organizer	Company Description ActiveSight uses an integrated Fragment-based Lead Discovery (FBLD) platform, LENS™, to develop tightly binding lead compounds quickly. LENS, or Lead Evolution via Novel Synergies, utilizes ActiveSight's expertise in structural biology, advanced binding detection methods, cutting edge diagnostics, automated software, and parallel chemistry to leverage the power of FBLD efficiently and effectively.
ActiveSight's FBLD Offerings	ActiveSight offers its partners an integrated and modular approach to Fragment-based Lead Discovery (FBLD), working together to generate tightly-binding lead compounds that are more likely to succeed in the clinic. By leveraging ActiveSight's LENS Technology, Partners can take advantage of cutting-edge FBLD technologies without the capital expenditure normally required. In addition, ActiveSight FBLD collaborations can be used as a proof of concept for obtaining the budget to fund future in-house FBLD equipment and programs
ActiveSight's FBLD 2008 Activities	Tuesday 1:00-2:00 p.m.	A demonstration of fragment screening protocols used at ActiveSight.
Premier Sponsor	Company Description ASDI Inc., established in 1988, is a premier provider of research-enabling technologies, services, and products. ASDI has considerable synthetic chemistry expertise in providing intermediate scale custom synthesis, hit-to-lead expansion, and lead generation libraries. Product lines include HTS, building block, and fragment screening collections. ASDI also offers complete bioanalytical and ADME/Tox services in support of early drug discovery. Our ability to provide analytical and materials management services enables acceleration of the research process.
ASDI's FBLD Offerings	Fragment Collections	In-house fragment libraries designed to maximize chemical space
	Fragment Procurement	Sourcing of third party collections
	Fragment Reformatting	Sample preparation for screening
	Inventory Management	Full services supporting storage, preparation, and distribution of fragments
Exhibitor	Company Description EMD, comprising of Calbiochem, Novabiochem, and Novagen brands, is engaged in the development, manufacture, marketing, and distribution of a broad array of research reagents used in life science research. The products these brands provide include tools for peptide synthesis, Proteomics and disease-related research.
Exhibitor	Company Description FUJIFILM Medical Systems USA, Inc. is a leading provider of medical and life science image, is a wholly owned U.S. subsidiary of FUJIFILM Corporation (FUJIFILM), Tokyo. FUJIFILM will use leading-edge, proprietary technologies to provide top-quality products and services that contribute to the advancement of culture, science, technology and industry, as well as improved health and environmental protection in society. Our overarching aim is to help enhance the quality of life of people worldwide.
Fujifilm's FBLD Offerings	AP-3000	Fully Automated, Label-Free Drug Screening System
Premier Sponsor	Company Description Biacore™ (now part of GE Healthcare) systems for label-free interaction analysis generate unique data on molecular interactions, giving insights into biological functions. Applications include drug discovery, life science research, antibody characterization, immunogenicity, biotherapeutic development and manufacturing.
GE Healthcare's FBLD Offerings	Biacore™ A100	Automated, high throughput system for label-free screening and characterization of drug-target interactions
	Biacore™ T100	Versatile, automated system for label-free analysis of drug-target interactions
Exhibitor	Company Description Graffinity Pharmaceuticals is a leader in the field of fragment based drug discovery. The Graffinity fragment screening platform combines chemical microarrays with a proprietary method for the standardized, label-free detection of compound-protein interactions via SPR imaging. The company's rapid and scalable drug discovery technology explores a rich chemical universe to identify drug fragments which address challenging drug targets. With its 110,000-compound library that contains 23,000 true fragments, Graffinity possesses one of the most diverse fragment libraries.
Graffinity's FBLD 2008 Activities	18 Feb 08, 1:45pm	Graffinity's SPR-based high throughput fragment screening Presentation: An introduction to Graffinity's small molecule fragment screening technology.
	18 Feb 08, 2:30pm	Graffinity drug discovery case studies Presentation: Case studies highlighting Graffinity's capabilities in screening protein-protein interaction targets, identifying allosteric binders as well as highly selective hits.
	19 Feb 08, 1:15pm	Graffinity's SPR-based high throughput fragment screening Presentation: An introduction to Graffinity's small molecule fragment screening technology.
	19 Feb 08 2:00pm	Graffinity drug discovery case studies Presentation: Case studies highlighting Graffinity's capabilities in screening protein-protein interaction targets, identifying allosteric binders as well as highly selective hits.
Exhibitor	Company Description IOTA Pharmaceuticals and Vitas-M Laboratories are collaborating to provide a complete FBLD tool kit for our customers, including project-based design of FBLD campaigns, provision of target-focused FBLD libraries, and the execution of FBLD screening and lead optimisation programs. The extensive medicinal chemistry and drug screening capabilities of the two companies, coupled to dedicated, proprietary FBLD resources, enable our customers to progress drug discovery programs to valuable "lead" endpoints in a reliable, cost-effective and efficient manner. Worked examples of such programs will be given at the conference.
IOTA/Vitas FBLD Offerings	Fragment Screening Collections	Over 5500 proprietary chemical fragments, optimized for screening, available today to IOTA-Vitas customers.
	Fragment Screening	Fragment screening on validated biochemical platforms available to IOTA-Vitas customers
Premier Sponsor	Company Description MicroCal is the leading developer of ultrasensitive calorimeters for the life sciences. For over thirty years, MicroCal Isothermal Titration Calorimeters and Differential Scanning Calorimeters have been used to characterize biomolecular interactions and structure. Microcalorimetry complements structural data and provides a sensitive, direct mode for determining binding affinities. The technique directly measures the heat of interaction, which is common to all binding processes. This removes the need for immobilization, labeling or specific assay design improving the biological relevance of data.
MicroCal's FBLD Offerings	VP-DSC	Differential Scanning Calorimeter
	CAPDSC	Capillary Differential Scanning Calorimeter
	ITC 200	Isothermal Titration Calorimetry
	Auto-ITC 200	Automated Isothermal Titration Calorimetry
Premier Sponsor	Company Description Nanosyn is a state-of-the-art chemistry contract research organization (CRO), providing a wide array of rapid and high quality chemistry products and services for the biotech and pharmaceutical industries worldwide. Products and services include: Medicinal Chemistry, Analytical Chemistry, Small Molecule X-Ray, Collaborative Projects and Research, "Plug & Play" Screening Libraries and Proprietary Library Development. In business since 1998, Nanosyn is conveniently located in the Biotech Hotbed communities of San Francisco and San Diego, California.
Nanosyn's FBLD Offerings	Chemistry On Demand™	Medicinal chemistry services to support fragment based lead discovery
	PureQuality™	High throughput LC/MS purification, compound analysis, quantitiation in screening buffer, and formating. PureQuality™ allows for rapid quality enhancement of your current fragment library or to support the production of new proprietary fragment libraries designed to maximize chemical space.
Nanosyn's FBLD 2008 Activities	Monday 8:00pm	"Chemistry on Demand" Approach to Support Fragment Based Lead Discovery. This presentation will describe Nanosyn's highly efficient technological processes based on heavy use of modern analytical and chemistry instrumentation. Case Studies will be presented.
	Tuesday 2:00pm	Nanosyn FBLD Case Studies. This presentation will describe case studies highlighting Nanosyn's medicinal chemistry capabilities allowing for the rapid and cost efficient support of fragment based lead discovery.
Exhibitor	Company Description QIAGEN offers the world's largest choice of over 2000 proven crystallization conditions, including JSCG Core Suites - 384 conditions giving the highest hit rates from over 500,000 high-throughput crystallization experiments at the Joint Center for Structural Genomics. Every condition is available as a large-volume Refill Hit, with certificated production reports ensuring reproducible and reliable crystallization for fragment-based or combinatorial library screening - applications further facilitated by the new EasyXtal 15-well Tool, whose SBS footprint makes it ideally suited for automatic visualization systems.
Qiagen's FBLD Offerings	EasyXtal 15-well Tool X-seal (20)	20 empty 15-well plates with X-Seal crystallization supports
	JCSG Core Suite I	Pierceable deep-well block containing 96 x 1.5 ml JCSH Core Suite I solutions, piercing tool, adhesive foil
	JCSG Core Suite II	Pierceable deep-well block containing 96 x 1.5 ml JCSH Core Suite II solutions, piercing tool, adhesive foil
	JCSG Core Suite III	Pierceable deep-well block containing 96 x 1.5 ml JCSH Core Suite III solutions, piercing tool, adhesive foil
	JCSG Core Suite IV	Pierceable deep-well block containing 96 x 1.5 ml JCSH Core Suite IV solutions, piercing tool, adhesive foil
Premier Sponsor	Company Description Rigaku is the world's leading provider of single crystal X-ray crystallographic hardware, software and contract services. We offer fully integrated macromolecular X-ray diffraction systems and modular protein crystallization systems for the automatic preparation of crystallization trials. The Rigaku product line includes imaging plate and CCD detectors, microfocus X-ray generators, X-ray optics, protein crystallization automation and imaging solutions, cryo-cooling devices, structure solution software and related peripherals.
Rigaku's FBLD Offerings	ACTOR™	The world's first commercial robotic system for automated crystal sample handling. Eliminates much of the physical handling of protein samples required during crystal screening and data collection.
	CrystalMation™	A fully integrated, configurable platform for protein crystallization, automating every step from custom screen making to crystallization trial imaging and analysis. Can be configured to meet a wide range of requirements and grow with your needs.
	MIFit+	Fully automated processing and structure solution tools that are ideal for fragment screening
	MtGUI	Bridges the information gap between crystallization and data collection and processing and includes full support for the new Rigaku RFID pins.
	Ultimate HomeLab™	Enables X-ray data collection on the widest range of protein samples, including crystals that diffract too weakly for standard home sources. Features state-of-the-art microfocus X-ray generator technology, Osmic™ optics, Rigaku imaging plate and CCD detectors, and an ACTOR™ crystal mounting robot to maximize productivity.
Rigaku's FBLD 2008 Activities	Mon 1:30 - 3:00pm Mon 7:00 - 9:00pm Tues 10:10 - 10:40am Tues 1:00 - 3:00pm	MtGUI Learn about MtGUI, new software for tracking crystal samples from the drop to data collection. This demonstration will also include the use of Rigaku RFID pins. ACTOR A demonstration of automated sample mounting hardware as well as software for scheduling, screening samples, data collection and processing. New developments for the ACTOR system and software will be presented.
Exhibitor	Company Description BIND© label free technology, from SRU Biosystems, represents a fundamental advance in the ability to monitor biological interactions by providing higher quality assay data with improved throughput and associated cost savings. The BIND© System can rapidly analyze the interactions of cells, proteins, genomic, peptide, antibody or small molecule compound libraries against a wide range of biochemical targets.
SRU Biosystems' FBLD Offerings	BIND Reader	High throughput, microplate based assay system that enables label-free detection of drug-target interactions
Exhibitor	Company Description Tripos International helps researchers in the pharmaceutical industry accelerate the identification and optimization of new compounds that have the potential to become drug products. Most new drugs start as a medicinal chemist's really good idea. AllChem, a new technology from Tripos, helps medicinal chemists find good new chemistry ideas that embody the best chances for the desired biological profile; structural novelty; a complete synthetic route; "drug-like-ness"; and hassle-free access
Tripos' FBLD Offerings	AllChem	Most new drugs start as a medicinal chemist's really good idea. AllChem, a new technology from Tripos, helps medicinal chemists find good new chemistry ideas that embody the best chances for the desired biological profile; structural novelty; a complete synthetic route; "drug-like-ness"; and hassle-free access.
Tripos' FBLD 2008 Activities	Mon. 1:30 - 3:00 pm Mon. 8:00 - 9:00 pm Tues. 1:00 - 3:00 pm	AllChem demonstration - learn how this new technology can help generate really good new chemistry ideas most likely to become leads. Submit your own structural queries and see the power of this exciting new techology!
Sponsor	Company Description ZoBio was founded in 2004 to make the Target Immobilized NMR Screening (TINS) technology available to the pharmaceutical and biotech world. ZoBio makes its TINS technology available primarily through fee-for-service offerings that with no restrictions on IP or royalties. A limited number of licensing opportunities are also available. ZoBio focuses exclusively on customer projects ZoBio has developed an innovative fragment library that is rule of three compliant (Siegal et al, Drug Discovery Today, 2007, 12, p.1032). The library is composed of commercially available compounds and is designed so that multiple analogs of each scaffold are readily available for follow-on studies. Screening of the library using TINS has been successfully applied to a number of challenging targets including kinases, small GTPases, molecular chaperones, viral enzymes, and membrane proteins. In all cases we have observed high rates of hit validation in biochemical assays and excellent success in crystallization studies.
ZoBio's FBLD Offerings	Fragment Screening	TINS screening of our innovative fragment collection using less than 5 mg of protein. TINS is a highly sensitive yet robust technology that typically enables "1st" site and "2nd site" discovery in a single screen. TINS screens are usually offered in conjunction with follow-on competition binding studies to determine ligand binding sites. Projects are typically completed in 1-2 months.
	Analoging	Follow up activity to develop SAR for hit scaffolds. Commercially available analogs are purchased and binding quantitated and characterized using TINS or other applicable methods.
	Hit Characterization	ZoBio has exclusive access to a solid state technology for biochemical characterization of kinases (S/T/Y) and nuclear hormone receptors. The technology can be used for rapid biochemical evaluation of TINS hits for e.g. potency, mode of action studies or profiling.
	Structure Determination of Target-Fragment Complexes	When X-ray crystallography is not applicable ZoBio can uses its expertise in NMR spectroscopy and computation to determine structures of fragments bound to the target. On the one hand rapid, low cost methods, such as chemical shift perturbation mapping; selective NOEs and paramagnetic relaxation enhancement, can be carried out to accurately map the ligand binding site to low resolution. On the other hand, full high resolution structure determination of target-fragment complexes is available.
ZoBio's FBLD 2008 Activities	Sun. 1:00 - 1:50 pm	Workshop Presentation: "The Use of NMR for Hit Detection and Evolution in FBLD"