Abstract
The application of NMR screening in drug discovery has recently attained heightened importance throughout the pharmaceutical industry. NMR screening can be applied at various points in a drug discovery program, ranging from very early in the program, when new targets can be screened long before an HTS enzymatic assay is developed, to later in the program, as in the case where no useful hits have been detected by HTS using biological assays. The binders determined in primary NMR screens are used to guide secondary screens, which can be either completely NMR driven or use NMR in combination with other biophysical techniques. In this review we briefly discuss the methods and techniques used in NMR screening. Then, we describe in detail the NMR screening strategies and their applications to specific targets, including successful examples from actual drug design programs at our own and other pharmaceutical companies.
Keywords: NMR Screening, HTS enzymatic assay
Current Topics in Medicinal Chemistry
Title: Application of NMR Screening in Drug Discovery
Volume: 3 Issue: 1
Author(s): Jasna Fejzo, Christopher Lepre and Xiaoling Xie
Affiliation:
Keywords: NMR Screening, HTS enzymatic assay
Abstract: The application of NMR screening in drug discovery has recently attained heightened importance throughout the pharmaceutical industry. NMR screening can be applied at various points in a drug discovery program, ranging from very early in the program, when new targets can be screened long before an HTS enzymatic assay is developed, to later in the program, as in the case where no useful hits have been detected by HTS using biological assays. The binders determined in primary NMR screens are used to guide secondary screens, which can be either completely NMR driven or use NMR in combination with other biophysical techniques. In this review we briefly discuss the methods and techniques used in NMR screening. Then, we describe in detail the NMR screening strategies and their applications to specific targets, including successful examples from actual drug design programs at our own and other pharmaceutical companies.
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Cite this article as:
Fejzo Jasna, Lepre Christopher and Xie Xiaoling, Application of NMR Screening in Drug Discovery, Current Topics in Medicinal Chemistry 2003; 3 (1) . https://dx.doi.org/10.2174/1568026033392796
DOI https://dx.doi.org/10.2174/1568026033392796 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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