| Literature DB >> 26061013 |
Florent Samain1, Torun Ekblad2, Gediminas Mikutis1, Nan Zhong3, Mauro Zimmermann4, Angela Nauer4,1, Davor Bajic4, Willy Decurtins4, Jörg Scheuermann4, Peter J Brown3, Jonathan Hall4, Susanne Gräslund3, Herwig Schüler2, Dario Neri4, Raphael M Franzini4.
Abstract
We describe the synthesis and screening of a DNA-encoded chemical library containing 76230 compounds. In this library, sets of amines and carboxylic acids are directly linked producing encoded compounds with compact structures and drug-like properties. Affinity screening of this library yielded inhibitors of the potential pharmaceutical target tankyrase 1, a poly(ADP-ribose) polymerase. These compounds have drug-like characteristics, and the most potent hit compound (X066/Y469) inhibited tankyrase 1 with an IC50 value of 250 nM.Entities:
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Year: 2015 PMID： 26061013 DOI： 10.1021/acs.jmedchem.5b00432
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446