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Article

Structure based design of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors from a phenotypic screen.

Bioorganic & medicinal chemistry letters - 1 Feb 2018

Palacios Daniel S, Meredith Erik, Kawanami Toshio, Adams Christopher, Chen Xin, Darsigny Veronique, Geno Erin, Palermo Mark, Baird Daniel, Boynton Geoffrey, Busby Scott A, George Elizabeth L, Guy Chantale, Hewett Jeffrey, Tierney Laryssa, Thigale Sachin, Weihofen Wilhelm, Wang Louis, White Nicole, Yin Ming, Argikar Upendra A

Abstract excerpt

Nicotinamide phosphoribosyltransferase is a key metabolic enzyme that is a potential target for oncology. Utilizing publicly available crystal structures of NAMPT and in silico docking of our internal compound library, a NAMPT inhibitor, 1, obtained from a phenotypic screening effort was replaced with a more synthetically tractable scaffold. This compound then provided an excellent foundation for further...

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Identifiers

PMID: 29275937
DOI: 10.1016/j.bmcl.2017.12.037

Genes

NAMPT

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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