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A new general approach for the simultaneous chemical synthesis of large numbers of oligonucleotides: Segmental solid supports
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A general and expedient method for the solid-phase synthesis of 1,4-benzodiazepine derivatives
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'Diversomers': An approach to nonpeptide nonoligomeric chemical diversity
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Peptoids: A modular approach to drug discovery
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Peptide microarrays for the determination of protease substrate specificity
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Salisbury CM, Maly DJ, Eliman JA: Peptide microarrays for the determination of protease substrate specificity. J Am Chem Soc (2002) 124(50):14868-14870. The first example of a fluorogenic peptide microarray.
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J Am Chem Soc
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Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries
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Harris JL, Backes BJ, Leonetti F, Mahrus S, Eliman JA, Craik CS: Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries. Proc Natl Acad Sci USA (2000) 97(14):7754-7759. An excellent report of the generation of fluorogenic peptide arrays and their use in profiling the substrate specificity of proteases.
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Proc Natl Acad Sci USA
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Carbohydrate arrays for the evaluation of protein binding and enzymatic modification
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Fabrication of carbohydrate chips for studying protein-carbohydrate interactions
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J Am Chem Soc
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Cheeseman, J.D.1
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Ge N, Cho SJ, Hermsmeier M, Poss M, Shen FC: Testing non-additivity of biological activity in a combinatorial library. Comb Chem High Throughput Screen (2002) 5(2):147-154. This paper is the first publication of the concept of additive analysis of combinatorial libraries.
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Comb Chem High Throughput Screen
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Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl) -2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors
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Willoughby CA, Hutchins SM, Rosauer KG, Dhar MJ, Chapman KT, Chicchi GG, Sadowski S, Weinberg DH, Patel S, Malkowitz L, Di Salvo J et al: Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors. Bioorg Med Chem Lett (2002) 12(1):93-96. This paper illustrates how a lead discovery library can be used to generate compounds that selectively target members within an entire receptor family.
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Bioorg Med Chem Lett
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Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands
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Cha MY, Choi BC, Kang KH, Pae AN, Choi KI, Cho YS, Koh HY, Lee HY, Jung D, Kong JY: Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands. Bioorg Med Chem Lett (2002) 12(10):1327-1330.
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Bioorg Med Chem Lett
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Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands
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Bleicher KH, Wüthrich Y, De Boni M, Kolczewski S, Hoffmann T, Sleight AJ: Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands. Bioorg Med Chem Lett (2002) 12(18):2519-2522.
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Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin-1 receptor ligands
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Bleicher KH, Wüthrich Y, Adam G, Hoffmann T, Sleight AJ: Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin-1 receptor ligands. Bioorg Med Chem Lett (2002) 12(21):3073-3076.
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Erythropoietin mimetics derived from solution phase combinatorial libraries
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Goldberg J, Jin Q, Ambroise Y, Satoh S, Desharnais J, Capps K, Boger DL: Erythropoietin mimetics derived from solution phase combinatorial libraries. J Am Chem Soc (2002) 124(4):544-555.
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Inhibitors of cell migration that inhibit intracellular paxillin/ α4 binding: A well-documented use of positional scanning libraries
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Ambroise Y, Yaspan B, Ginsberg MH, Boger DL: Inhibitors of cell migration that inhibit intracellular paxillin/α4 binding: A well-documented use of positional scanning libraries. Chem Biol (2002) 9(11):1219-1226. This paper provides an interesting comparison between the traditional mixture-based library approach and a positional scanning strategy.
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Chem Biol
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Urbahns K, Härter M, Albers M, Schmidt D, Stelte-Ludwig B, Brüggemeier U, Vaupel A, Gerdes C: Biphenyls as potent vitronectin receptor antagonists. Bioorg Med Chem Lett (2002) 12(2):205-208.
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Bioorg Med Chem Lett
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Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase
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Haque TS, Tadesse S, Marcinkeviciene J, Rogers MJ, Sizemore C, Kopcho LM, Amsler K, Ecret LD, Zhan DL, Hobbs F, Slee A et al: Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase. J Med Chem (2002) 45(21):4669-4678. An iterative library design coupled with a strategy to explore additive/non-additive SAR trends allows the discovery of potent lead molecules.
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J Med Chem
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Synthesis and optimization of a new family of type 3 17β-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry
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Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design
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Choong IC, Lew W, Lee D, Pham P, Burdett MT, Lam JW, Wiesmann C, Luong TN, Fahr B, DeLano WL, McDowell RS et al: Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design. J Med Chem (2002) 45(23):5005-5022.
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J Med Chem
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Choong, I.C.1
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Potent, novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC
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Kline T, Andersen NH, Harwood EA, Bowman J, Malanda A, Endsley S, Erwin AL, Doyle M, Fong S, Harris AL, Mendelsohn B et al: Potent, novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC. J Med Chem (2002) 45(14):3112-3129.
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J Med Chem
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Kline, T.1
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Solid-phase synthesis and biological evaluation of a pepticinnamin E library
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Thutewohl M, Kissau L, Popkirova B, Karaguni IM, Nowak T, Bate M, Kuhlmann J, Müller O, Waldmann H: Solid-phase synthesis and biological evaluation of a pepticinnamin E library. Angew Chem Int Ed (2002) 41(19):3616-3620. A library evaluation leads to the identification of several compounds with different binding modes from the same lead structure.
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Angew Chem Int Ed
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Thutewohl, M.1
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0037076419
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Anticonvulsant activity of a nonpeptide galanin receptor agonist
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Proc Natl Acad Sci USA
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Saar, K.1
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High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists
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Finn J, Pelham D, Walker MW, Gluchowski C: High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists. Bioorg Med Chem Lett (2002) 12(13):1771-1774.
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Bioorg Med Chem Lett
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A combinatorial library of indinavir analogues and its in vitro and in vivo studies
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Cheng Y, Rano TA, Huening TT, Zhang F, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Kuo LC, Lin JH et al: A combinatorial library of indinavir analogues and its in vitro and in vivo studies. Bioorg Med Chem Lett (2002) 12(4):529-532. Pools of compounds from a mixture-based library are administered to dogs, resulting in the identification of potent compounds with better pharmacokinetic properties than indinavir.
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Bioorg Med Chem Lett
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Cheng, Y.1
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An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors
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McKenna JM, Halley F, Souness JE, McLay IM, Pickett SD, Collis AJ, Page K, Ahmed I: An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors. J Med Chem (2002) 45(11):2173-2184.
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J Med Chem
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McKenna, J.M.1
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Ahmed, I.8
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