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Merck

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.

Journal of medicinal chemistry (2017-11-21)
Upendra Rao Anumala, Jo Waaler, Yves Nkizinkiko, Alexander Ignatev, Katina Lazarow, Peter Lindemann, Petter Angell Olsen, Sudarshan Murthy, Ezeogo Obaji, Alexander G Majouga, Sergey Leonov, Jens Peter von Kries, Lari Lehtiö, Stefan Krauss, Marc Nazaré
RESUMO

A structure-guided hybridization approach using two privileged substructures gave instant access to a new series of tankyrase inhibitors. The identified inhibitor 16 displays high target affinity on tankyrase 1 and 2 with biochemical and cellular IC

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Cyclobutanecarbohydrazide, AldrichCPR
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