The Design of Leadlike Combinatorial Libraries

The Design of Leadlike Combinatorial Libraries

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 sc...

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Bibliographic Details
Published in:Angewandte Chemie International Edition Vol. 38; no. 24; pp. 3743 - 3748
Main Authors: Teague, Simon J., Davis, Andrew M., Leeson, Paul D., Oprea, Tudor
Format: Journal Article
Language:English
Published: Weinheim WILEY-VCH Verlag GmbH 16-12-1999
WILEY‐VCH Verlag GmbH
Subjects:
Bioorganic chemistry
Combinatorial chemistry
Drug research
Structure-activity relationships
Online Access:Get full text
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Summary: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.
Bibliography:istex:E7B7C1240F520C9708D8A024FBE0603129D4CB5C
ark:/67375/WNG-3C7N0X2R-0
ArticleID:ANIE3743
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1433-7851
1521-3773
DOI:10.1002/(SICI)1521-3773(19991216)38:24<3743::AID-ANIE3743>3.0.CO;2-U