Artigo Revisado por pares

The Design of Leadlike Combinatorial Libraries

1999; Wiley; Volume: 38; Issue: 24 Linguagem: Inglês

10.1002/(sici)1521-3773(19991216)38

ISSN

1521-3773

Autores

Simon J. Teague, A. M. Davis, Paul D. Leeson, Tudor I. Oprea,

Tópico(s)

Click Chemistry and Applications

Resumo

Angewandte Chemie International EditionVolume 38, Issue 24 p. 3743-3748 Communication The Design of Leadlike Combinatorial Libraries Simon J. Teague, Simon J. Teague [email protected] Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorAndrew M. Davis, Andrew M. Davis Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorPaul D. Leeson, Paul D. Leeson Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorTudor Oprea, Tudor Oprea Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this author Simon J. Teague, Simon J. Teague [email protected] Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorAndrew M. Davis, Andrew M. Davis Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorPaul D. Leeson, Paul D. Leeson Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this authorTudor Oprea, Tudor Oprea Department of Medicinal Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH (UK), Fax: (+44) 1509-645-571Search for more papers by this author First published: 16 December 1999 https://doi.org/10.1002/(SICI)1521-3773(19991216)38:24 3.0.CO;2-UCitations: 576AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Abstract The optimization of low-potency leads into drugs is often accompanied by an increase in molecular weight (Mr) and lipophilicity, as a consequence of affinity enhancement. Hits with affinity at μM levels discovered by screening leadlike libraries allow scope for this optimization process, as shown schematically by the distributions of Mr for a leadlike library (1), oral drugs (2), and a typical combinatorial chemistry library (3). y=percentage with a particular molecular weight. Citing Literature Volume38, Issue24December 16, 1999Pages 3743-3748 RelatedInformation

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