Literature DB >> 26733476

Salicylates are interference compounds in TR-FRET assays.

Ronan P Hanley1, Shanti Horvath1, Jianghong An2, Fraser Hof1, Jeremy E Wulff1.   

Abstract

Given the importance of high-throughput screening in drug discovery, the identification of compounds that interfere with assay readouts is crucial. The pursuit of false positives wastes time and money, while distracting development teams from more promising leads. In the context of TR-FRET assays, most interfering compounds are dyes or aggregators. In the course of our studies on the PD1-PDL2 interaction, we discovered that salicylic acids, an extremely common compound subclass in screening libraries, interfere with TR-FRET assays. While the precise mechanism of interference was not established, our data suggest that interaction of the salicylate with the cryptand-ligated europium FRET donor is responsible for the change in assay signal.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Assay development; Interference compounds; PAINS; Salicylates; TR-FRET

Mesh:

Substances:

Year:  2015        PMID: 26733476     DOI: 10.1016/j.bmcl.2015.12.050

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  In Vitro Assessment of Putative PD-1/PD-L1 Inhibitors: Suggestions of an Alternative Mode of Action.

Authors:  Derek J Blevins; Ronan Hanley; Trevor Bolduc; David A Powell; Michael Gignac; Kayleigh Walker; Mark D Carr; Fraser Hof; Jeremy E Wulff
Journal:  ACS Med Chem Lett       Date:  2019-07-02       Impact factor: 4.345

2.  Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015).

Authors:  Tryfon Zarganes-Tzitzikas; Markella Konstantinidou; Yongzhi Gao; Dobroslawa Krzemien; Krzysztof Zak; Grzegorz Dubin; Tad A Holak; Alexander Dömling
Journal:  Expert Opin Ther Pat       Date:  2016-07-06       Impact factor: 6.674

Review 3.  Seven Year Itch: Pan-Assay Interference Compounds (PAINS) in 2017-Utility and Limitations.

Authors:  Jonathan B Baell; J Willem M Nissink
Journal:  ACS Chem Biol       Date:  2017-12-26       Impact factor: 5.100

  3 in total

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