期刊
ACS COMBINATORIAL SCIENCE
卷 17, 期 1, 页码 49-59出版社
AMER CHEMICAL SOC
DOI: 10.1021/co500154e
关键词
rapid lead discovery; iterative screening; one bead one compound (OBOC) libraries; structure-activity relationship (SAR)
资金
- NHLBI [NO1-HV-00242]
Primary hits that arise from screening one bead one compound (OBOC) libraries against a target of interest rarely have high potency. However, there has been little work focused on the development of an efficient workflow for primary hit improvement. In this study, we show that by characterizing the binding constants for all of the hits that arise from a screen, structure-activity relationship (SAR) data can be obtained to inform the design of derivative libraries of a primary hit that can then be screened under more demanding conditions to obtain improved compounds. Here, we demonstrate the rapid improvement of a primary hit against matrix metalloproteinase-14 using this approach.
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