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relating to combinatorial chemistry. We offer our apologies to those companies or products that were inadvertently omitted from this listing.

The information provided was obtained from various public sources, including company press releases, company internet web sites, articles appearing in many of the industry trade journals, magazines, product advertising, product brochures, and other company sources. The entries contain information available at the time the chapter was written and are as accurate as the original sources. A listing of a company or its products does not constitute an endorsement.

Abbott Laboratories

100 Abbott Park Road, Abbott Park, IL 60064-3500, USA Phone: [phone]; Fax: [phone]

Toll-free in U.S.: [phone] Internet: http:/ /www.abbott.com

Stock: ABT (NYSE)

Profile: One of the world’s leading health care companies, Abbott is dedicated to improving people’s lives through the discovery, development, manufacture, and marketing of health care products and services. Its strategy is to provide innovative technologies that improve the quality of health care while helping customers lower their costs.

Products/technologies: A team of scientists developed what they consider a revolutionary technique for discovering new drugs that could potentially have far-reaching implications for disease management. Called SAR by NMR (Structure–Activity Relationships by Nuclear Magnetic Resonance), Abbott claims the technique can significantly speed the difficult and time-consuming process for identifying molecules that bind to important protein drug targets.

Abbott compares SAR by NMR to combinatorial chemistry as follows: Both methods use a building block approach in the construction of molecules; however, in combinatorial chemistry, thousands to millions of molecules are typically synthesized and tested for activity. In SAR by NMR, less than 10 molecules is required because the chemistry is highly focused on linking molecules demonstrated to bind to the protein target using structural information on how they interact. Patent applications have been filed on the method, but the company plans to make the technology available to other drug developers.

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Contact: Ellen Molleston Walvoord, V.P., Investor Relations and Public Affairs

Acacia Bioscience

4136 Lakeside Drive, Richmond, CA 94806, USA Phone: [phone]; Fax: [phone] E-mail: [e-mail]

Internet: http:/ /www.acaciabio.com

Profile: Acacia Bioscience is a functional genomics and drug discovery company using advances in genome science and combinatorial chemistry to identify potential lead compounds with higher degrees of therapeutic value.

Products/technologies: Acacia’s drug discovery technology, called the Genome Reporter Matrix , screens molecules against multiple intracellular disease pathways, revealing the in vivo targets of compounds with therapeutic value and increasing the efficiency of the drug discovery process. The Matrix can be used to enhance the screening of combinatorial libraries, detect the potential side effects of a drug candidate, resurrect failed drug candidates, and accelerate the discovery of new drug leads.

Contact: Bruce Cohen, President and CEO

ACADIA Pharmaceuticals

3911 Sorrento Valley Blvd., San Diego, CA 92121, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.acadia-pharm.com

Profile: ACADIA Pharmaceuticals is a biotechnology company engaged in development and use of high-throughput solutions for drug discovery. Founded in 1993, the company has developed a platform of proprietary breakthrough technologies for the functional characterization of genes encoding potential drug targets. ACADIA pursues drug discovery alliances with major pharmaceutical firms, as well as with biotechnology companies with expertise in genomics and combinatorial chemistry. It continues to develop and expand its technology platform and in-house discovery efforts on novel targets. Research facilities are maintained in both San Diego and Copenhagen, Denmark.

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The company changed its name in August 1997 from Receptor Technologies Inc., and moved from Winooski, Vermont, to its California location.

Products/technologies: It has developed a proprietary technology that is referred to as Receptor Selection and Amplification Technology (R-SAT ). R-SAT permits the assaying of drug activity using recombinant receptors. The R-SAT assay is a high throughput assay that can be performed with a wide range of receptors that use a diversity of signal transduction mechanisms. The company claims that precise quantitative data for agonist, partial agonists, as well as neutral antagonists and negative antagonists (inverse agonists) can be obtained. Company offers contract assays, mass screening, reagents, and a novel method for expression cloning based on the R-SAT assay.

Contact: Mark R. Brann, Ph.D., CEO and Chief Scientific Officer

Advanced ChemTech

5609 Fern Valley Road, Louisville, KY 40228-1075, USA Phone: [phone]; Fax: [phone]

Toll-free in U.S.: [phone] E-mail: [e-mail] Internet: http:/ /www.peptide.com

Profile: A manufacturer of synthesis instrumentation, biochemicals, and life science products, the company is a pioneer in the field of multiple synthesis technology. It manufactures a diverse line of instrumentation with applications in molecular diversity and rational design for drug discovery and development, including commercial models for high throughput organic small molecule and mixture combinatorial synthesis, as well as numerous proprietary synthesizer models. In addition to its headquarters in Kentucky, subsidiaries and distributors are located in Europe, Japan, Singapore/Southeast Asia, Korea, China/ Hong Kong, India, and Taiwan.

Products/technologies: These include the BenchMark Synthesis series of combinatorial and high-throughput organic synthesis systems (384 HTS, 496 MOS, 440 MOS); ReacTech organic synthesizer; plus other instrumentation for combinatorial peptide and organic synthesis; catalog of peptide libraries, custom peptides, and peptide library synthesis services; extensive selection of amino acid derivatives, solid supports reagents, and other starting materials

for solid phase organic, peptide, and combinatorial synthesis. The ACT Model 496 Multiple Organic Synthesizer is a fully automated dual-arm robotics

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synthesizer that can make up to 96 different compounds in a single run; reaction blocks with 40, 16, and 8 wells are also available. The ACT Model 357 FBS can be used in automated single or multiple organic and bioorganic molecular synthesis. It can synthesize up to 36 different compounds and can serve as a large-scale, single-product synthesizer with scales of up to 36 g or more of starting resin. Combinatorial libraries can also be prepared by the split-pool method.

Contact: Mark L. Peterson, Ph.D.

Afferent Systems, Inc.

440 Collingwood St., San Francisco, CA 94114, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.afferent.com

Profile: The company develops software for combinatorial chemistry, including instrument control, and product data generation, storage, and access. It also offers solution phase and solid phase combinatorial synthesis instruments that are low cost and offer a high throughput. Software runs on PCs under Windows 95 and NT 4.0 and on SGI workstations. Free short-term evaluation licenses are offered for those interested in evaluating the software.

Products/technologies: Myriad integrated system for combinatorial chemistry informatics combines multiple functional modules under a single graphical user interface. The first three modules are a combinatorial database generator, combinatorial database engine and browser, and a synthetic instrument controller. The Afferent synthesis station is based on Myriad, the Gilson 215 liquid handler, and optionally the Charybdis Calypso reaction block.

Affymax

4001 Miranda Ave., Palo Alto, CA 94304, USA Phone: [phone]; Fax: [phone] E-mail: [e-mail]

Internet: http:/ /www.affymax.com

Profile: Affymax is a wholly owned subsidiary of Glaxo Wellcome.

Products/technologies: ESL (Encoded Synthetic Library) technology enables the identification of individual organic compounds from combinatorial librar-

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ies containing hundreds to hundreds of thousands of such compounds. Using ESL, a scientist can synthesize a large library of compounds in combinatorial mixtures, attaching tags at each reaction step. When an active compound is found, the tags allow the scientist to readily identify the specific active structure.

Contact: Gordon Ringold, Ph.D., CEO and Scientific Director, Affymax Research Institute

Affymetrix

3380 Central Expressway, Santa Clara, CA 95051, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.affymetrix.com

Stock: AFFX (NASDAQ)

Profile: Affymetrix started operations in 1991 as a division of Affymax, N.V. and began operating independently as a wholly owned subsidiary of Affymax in February 1993. In March 1995, Glaxo Wellcome purchased Affymax, including its then 65% interest in Affymetrix. As a result of subsequent financings, Glaxo Wellcome’s ownership was approximately 34% of Affymetrix as of August 1997. The company has approximately 150 employees.

Products/technologies: The company’s GeneChip technology has potential for genomic applications—including linkage, association studies, and DNA fingerprinting. A collaboration agreement with Whitehead Institute in Cambridge, Massachusetts is focused on the development of a set of single-nucleo- tide polymorphic (SNP) markers that can be scored on a microchip—this could have uses in studies on gene expression or as a diagnostic screening tool to identify even single-point gene mutations.

Alanex Corporation

3550 General Atomics Ct., San Diego, CA 92121, USA Phone: [phone]; Fax: [phone]

Profile: Alanex began operations as a limited partnership in May 1991. In 1993 the partnership was converted to a California corporation. Alanex was acquired in May 1997 and operates as a privately held subsidiary of Agouron

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Pharmaceuticals (traded as AGPH on NASDAQ). The company is involved in the discovery and optimization of small-molecule drugs using its proprietary combinatorial chemistry, computational chemistry, high-throughput screening, and integrated information management system. An important element of the company’s strategy is to enter into collaborations with pharmaceutical companies.

Products/technologies: Alanex has developed and integrated its proprietary ChemInformatics system with combinatorial chemistry and high throughput screening. This combined approach is designed to significantly shorten the time required to find lead compounds and optimize them into viable drug candidates. Its proprietary core drug discovery technology, Pharmacophore Directed Parallel Synthesis (PDPS), combines combinatorial chemistry with computational and medicinal chemistries that, when used in conjunction with high-throughput screening and pharmacology, form an integrated drug discovery platform that can be broadly applied to a wide array of biological targets. Its proprietary library design software, LiBrain, is used to maximize the diversity of its exploratory library by selecting for synthesis compounds from Alanex’s virtual library of chemical structures.

Contact: Ed Baracchini, Ph.D.

Amersham Pharmacia Biotech

Bjorkgatan 30, S-751 82 Uppsala, Sweden

Phone: [phone]; Fax: [phone] Internet: http:/ /www.apbiotech.com

Stock: Parent companies listed as PH&U on Stockholm Stock Exchange; and PNU (NYSE)

Profile: In 1997 Amersham International plc and Pharmacia & Upjohn, Inc. merged their life science businesses, Amersham Life Science and Pharmacia Biotech, creating the world’s largest research-based biotechnology supplier. With over $700 million in combined annual sales and more than 3600 employees, the company will focus on lab and industrial chromatography, industrial DNA synthesis, high throughput drug screening, custom radiochemical synthesis, molecular biology reagents, DNA sequencing and mapping, and electrophoresis. The new company will focus R&D efforts on technologies for matrix/polymer chemistry, high throughput sequencing, drug screening, and microarrays.

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Products/technologies: The SMART System is optimized for micropurification and microbore chromatography. It recovers and purifies biologically active material present in subnanogram, nanogram, and picogram amounts. By scaling down column dimensions and optimizing system components, it delivers the low volumes and high concentrations of pure biologically active substances that life science researchers need for further investigation by microanalytical techniques. It is also used in peptide sequencing and protein structure–function applications. The company, along with Molecular Dynamics, developed a microarray system that permits researchers to make and analyze high-density microarrays with increased speed, efficiency, and sensitivity. Data from a single microarray experiment provide researchers with the ability to accurately measure gene expression levels in thousands of samples. In late 1996 the two companies launched the Microarray Technology Access Program to make available preferential, precommercial access to their microarray technology.

Contact: Mike Evans, Vice President

Argonaut Technologies

887 Industrial Road, Suite G, San Carlos, CA 94070, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.argotech.com

Profile: Argonaut was incorporated in November 1994 and completed a firstround venture financing of $4.5 million in January 1995. A second-round venture financing of $9.5 million was completed in May 1996. In addition to the research and development facility the company occupies in San Carlos, California, it also has facilities in Tucson, Arizona, and Basel, Switzerland, as well as a distributor in Japan.

Products/technologies: The company designs and develops a full range of instruments, reagents, consumables, and software that apply solid phase technologies to the synthesis and purification of small organic molecules. Products are aimed at improving the productivity of the medicinal chemistry laboratory by exploiting the vast productivity gains derived from high-speed parallel synthesis and combinatorial chemistry. Products include ArgoGel resins and ArgoPore resins for solid phase synthesis. The Nautilus 2400 Organic Synthesizer handles complex reactions, has the flexibility to synthesize small molecules using a broad range of chemistries, and handles a wide range of reagents, with capability for temperature control and use of inert atmospheres. The Quest

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210 manual synthesizer can run up to 20 parallel reactions and can be used for solid or solution phase chemistries in a wide range of synthesis applications.

Contact: David P. Binkley, Ph.D., President and CEO

ArQule, Inc.

200 Boston Avenue, Suite 3600, Medford, MA 02155, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.arqule.com

Stock: ARQL (NASDAQ)

Profile: ArQule was started in 1993 and completed its IPO in October 1996. The company created a technology platform for the discovery and production of chemical compounds with commercial potential, and provides novel compounds to the pharmaceutical and biotechnology industries.

Products/technologies: Proprietary modular building block technology integrates structure-guided drug design, high-speed parallel chemical synthesis; and information technology to accelerate the identification and optimization of drug development candidates. The company’s Mapping Array products are proprietary libraries of novel, diverse, small-organic-molecule compounds used for screening against biological targets in lead generation. Directed Array products are customized libraries of closely related compounds for lead optimization. Products are based on a technology platform composed of structure-guided drug design, modular building block chemistry, combinatorial chemistry, informatics, and the company’s Automated Molecular Assembly Plant (AMAP ). Scalability of products enables the development process to accelerate directly into the lead optimization phase.

Contact: Eric B. Gordon, M.D., President and CEO

Aurora Biosciences Corporation

11149 N. Torrey Pines Road, La Jolla, CA 92037, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.auroabio.com

Stock: ABSC (NASDAQ)

Profile: Founded in 1995, Aurora’s primary mission is to advance drug discovery by developing miniaturized, automated systems for ultrahigh-throughput

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screening based on proprietary, versatile, fluorescence-based assays. The company was incorporated in California in May 1995 and reincorporated in Delaware in January 1996. The company announced its initial public offering of common stock in June 1997.

Products/technologies: Designs and develops proprietary drug discovery systems, services, and technologies to accelerate and enhance the discovery of new medicines. These systems enable very rapid screening of multiple genomic and other molecular targets to quickly and economically identify lead compounds with novel therapeutic potential. Aurora is developing an integrated technology platform comprising a portfolio of proprietary fluorescent assay technologies and an ultrahigh-throughput screening system designed to

allow assay miniaturization. According to the company, their ultrahighthroughput screening system (UHTSS ) can handle hundreds of thousands

of compounds every 24 hours.

Contact: Paul Grayson, Vice President, Corporate Development

Axiom Biotechnologies Inc.

3550 General Atomics Court, San Diego, CA 92121-1194, USA Phone: [phone]; Fax: [phone]

E-mail: [e-mail] Internet: http:/ /www.axiombio.com

Profile: A privately held company established in August 1995, Axiom is a drug discovery company that provides pharmaceutical companies with novel high-throughput pharmacology systems to accelerate the process of drug discovery. Axiom serves the pharmaceutical industry by offering access to its novel systems through research collaborations. In such collaborations Axiom provides research and development expertise, and technology transfer of its proprietary high-throughput pharmacology systems, including instrumentation, cell-based assays, laboratory information management systems, and analytical pharmacoinformatics tools, to accelerate in-house discovery efforts.

Products/technologies: These include the High Throughput Pharmacology System (HT-PS) for drug discovery that uses natural cell lines, which more closely simulate the body’s environment, to test compounds for a desired drug activity. The system consists of novel high-throughput pharmacology

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instrumentation, high-sensitivity cell-based assays, and novel pharmacoinformatics tools for managing and mining high-throughput pharmacology experimental data. Complementing Axiom’s HT-PS system is its LIMS system, built on an ORACLE platform that can be customized to meet individual labs’ needs.

Contact: James P. Linton, Senior Director, Business Development

AXYS Pharmaceuticals, Inc.

180 Kimball Way, South San Francisco, CA 94080, USA Phone: [phone]; Fax: [phone]

Internet: http:/ /www.axyspharm.com

Stock: AXPH (NASDAQ)

Profile: AXYS is involved in the integration of drug discovery technologies from gene identification through clinical development and is focused on the discovery of small-molecule therapeutics.

Products/technologies: Formerly Arris Pharmaceutical Corp., the company announced in January 1998 its plans to commercialize its capabilities in combinatorial chemistry and pharmacogenomics as well as its patented technology. The company licenses its combinatorial chemistry technology to pharmaceutical and biotech companies, and collaborates with companies wishing to screen its libraries.

Contact: Daniel Petree

Beckman Coulter, Inc.

2500 Harbor Blvd. Fullerton, CA 92834-3100, USA Phone: [phone]; Fax: [phone] Internet: http:/ /www.beckman.com

Stock: BEC (NYSE)

Profile: Founded in 1935, the company develops, manufactures, and markets automated systems and supplies for life science research and clinical diagnostic laboratories. Through its acquisition of Sagian, Beckman gained access to high-throughput screening technology and liquid-handling robotics instrumen-