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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Competition Binding Experiments for Rapidly Ranking Lead Molecules for their Binding Affinity to Human Serum Albumin

Author(s): Claudio Dalvita, Maria Flocco, Brian J. Stockman and Marina Veronesi

Volume 5, Issue 8, 2002

Page: [645 - 650] Pages: 6

DOI: 10.2174/1386207023329905

Price: $65


Many lead molecules that have high affinity for a therapeutic target in vitro exhibit a reduced efficacy in vivo. Drug binding to human serum albumin is a major contributor to this reduction in potency, and many drug discovery programs expend significant resources preparing compounds that have decreased albumin binding. As rational and structure-based approaches have already been demonstrated to design compounds that have reduced affinity for albumin, the ability to rapidly and accurately assess protein binding will be valuable in lead optimization. This review will summarize some of the NMR-based efforts towards developing universal, rapid, accurate, and site-specific assays for estimating protein binding.

Keywords: ligand-based NMR screening, High-Throughput Screening, HAS, Human Serum Albumin, dissociation binding constant, competition binding experiments, drug discovery

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