Comprehensive survey of chemical libraries yielding enzyme inhibitors, receptor agonists and antagonists, and other biologically active agents: 1992 through 1997

Roland E. Dolle
Department of Chemistry, Pharmacopeia, Inc., 101 College Road East, Princeton, NJ 08540, U.S.A.
E-mail: roland@pharmacop.com

Abstract
This review is a historical accounting of chemical libraries from which biologically active agents have been obtained. The comprehensive tabulation includes citations as early as 1992, when the first descriptions of biologically active libraries were disclosed, and continues through 1997. Four tables are provided listing libraries screened against (1) proteolytic enzymes, (2) non-proteolytic enzymes, (3) G-protein coupled receptors (GPCRs), and (4) other targets not classified in the first three tables (e.g., non-GPCRs, integrins, antiinfectives). A name, generic structure, and size is provided for each library citation, accompanied by the molecular screen and the structure and potency of the most active library member. In total, 86 libraries are presented with 60% of the contributions reported from pharmaceutical and biotechnology companies. Approximately 70% of the libraries have used a-amino acid synthons in their construction and 85% of the libraries include one or more amide bonds.

Keywords
agonist, antagonist, antiinfective, combinatorial chemistry, enzyme, inhibitor, kinase, protease, receptor