Two Comparisons of the Performance of Positional Scanning and Deletion Synthesis for the Identification of Active Constituents in Mixture Combinatorial Libraries
- 28 January 2000
- journal article
- research article
- Published by American Chemical Society (ACS) in The Journal of Organic Chemistry
- Vol. 65 (5) , 1467-1474
- https://doi.org/10.1021/jo9916481
Abstract
Two libraries of 120 compounds each were prepared as individual compounds and as full mixtures. The corresponding scanning and deletion synthesis deconvolution libraries were prepared and tested (L-1210, IC50) alongside the individual compounds and mixture libraries. This testing, where the properties of each compound in the mixtures were known, was used to compare the performance of scanning and deletion deconvolution libraries. Each has its own intrinsic strengths, with the former being capable of identifying multiple hits at the expense of accurately identifying the most potent library member, while the latter typically is more sensitive to identifying the most potent hit but at the expense of differentiating weaker activities. The protocols complement one another and together more thoroughly identify potent library members.Keywords
This publication has 20 references indexed in Scilit:
- Discovery of Potent Nonpeptide Vitronectin Receptor (αVβ3) AntagonistsJournal of Medicinal Chemistry, 1997
- Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregationBioorganic & Medicinal Chemistry Letters, 1996
- RGD AND OTHER RECOGNITION SEQUENCES FOR INTEGRINSAnnual Review of Cell and Developmental Biology, 1996
- Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin AntagonistsJournal of Medicinal Chemistry, 1996
- Non-peptide fibrinogen receptor antagonists. 3. design and discovery of a centrally constrained inhibitorBioorganic & Medicinal Chemistry Letters, 1994
- The pharmacology of the integrinsMedicinal Research Reviews, 1994
- Arginyl-glycyl-aspartic acid (RGD): a cell adhesion motifTrends in Biochemical Sciences, 1991
- Adhesion receptors of the immune systemNature, 1990
- New Perspectives in Cell Adhesion: RGD and IntegrinsScience, 1987
- Arg-Gly-Asp: A versatile cell recognition signalCell, 1986