Issue 2, 2016
From the journal:

MedChemComm

Focus on PAINS: false friends in the quest for selective anti-protozoal lead structures from Nature?†

J. Glasera  and  U. Holzgrabe*a  

* Corresponding authors

a Institute of Pharmacy and Food Chemistry, University of Wuerzburg, Am Hubland, 97074 Wuerzburg, Germany
E-mail: ulrike.holzgrabe@uni-wuerzburg.de

Abstract

Pan-assay interference compounds (PAINS) are molecules showing promising but deceptive activities in various biochemical screenings mainly due to unselective interactions with the target. Overall awareness of this problem has been raised recently. Many natural products inherently have PAINS characteristics but are nevertheless uncritically acclaimed as new antiprotozoal lead structures. However, a non-selective mode of action may be the cause of observed activity. This review describes the most common assay-interfering characteristics of antiprotozoal natural products, discusses significant examples from the recent literature and strategies to deal with these promiscuous structures.

Graphical abstract: Focus on PAINS: false friends in the quest for selective anti-protozoal lead structures from Nature?

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Article information

DOI
https://doi.org/10.1039/C5MD00481K
Article type
Review Article
Submitted
16 Oct 2015
Accepted
28 Dec 2015
First published
04 Jan 2016

Med. Chem. Commun., 2016,7, 214-223

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Focus on PAINS: false friends in the quest for selective anti-protozoal lead structures from Nature?

J. Glaser and U. Holzgrabe, Med. Chem. Commun., 2016, 7, 214 DOI: 10.1039/C5MD00481K

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