Angewandte Chemie International Edition
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Communication
The Design of Leadlike Combinatorial Libraries
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.