Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library

Journal of Medicinal Chemistry

Volumn 58, Issue 12, 2015, Pages 5143-5149

  Samain, Florent ^c   Ekblad, Torun ^b   Mikutis, Gediminas ^c   Zhong, Nan ^d   Zimmermann, Mauro ^a   Nauer, Angela ^a,c   Bajic, Davor ^a   Decurtins, Willy ^a   Scheuermann, Jörg ^a   Brown, Peter J ^d   Hall, Jonathan ^a   Gräslund, Susanne ^d   Schüler, Herwig ^b   Neri, Dario ^a   Franzini, Raphael M ^a  

^a ETH ZURICH   (Switzerland)

^b KAROLINSKA INSTITUTE   (Sweden)

^c PHILOCHEM AG   (Switzerland)

^d UNIVERSITY OF TORONTO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

AMINE; CARBOXYLIC ACID; DNA; TANKYRASE; TANKYRASE 1; TANKYRASE INHIBITOR; UNCLASSIFIED DRUG; [2 (2,4 DIOXOTETRAHYDROPYRIMIDIN 1(2H) YL) N PHENETHYLBENZAMIDE]; [N (4 BROMOPHENETHYL) 2 (2,4 DIOXOTETRAHYDROPYRIMIDIN 1(2H) YL)BENZAMIDE]; [N (4 CHLOROPHENETHYL) 2 (2,4 DIOXOTETRAHYDROPYRIMIDIN 1(2H) YL)BENZAMIDE]; [N [4 (1H PYRAZOL 1 YL)BENZYL] 2 (2,4 DIOXOTETRAHYDROPYRIMIDIN 1 (2H) YL) N METHYLBENZAMIDE]; ENZYME INHIBITOR; MOLECULAR LIBRARY; TNKS PROTEIN, HUMAN;

ARTICLE; BINDING AFFINITY; CHEMICAL STRUCTURE; CRYSTALLIZATION; DNA LIBRARY; DRUG SYNTHESIS; ENZYME INHIBITION; IC50; SCREENING; ANTAGONISTS AND INHIBITORS; CHEMISTRY; GENE LIBRARY; HUMAN; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY;

AMINES; CARBOXYLIC ACIDS; ENZYME INHIBITORS; GENE LIBRARY; HUMANS; MODELS, MOLECULAR; SMALL MOLECULE LIBRARIES; TANKYRASES;

EID: 84933059417     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00432     Document Type: Article

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