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. 2020 Jan 23;63(2):601-612.
doi: 10.1021/acs.jmedchem.9b01460. Epub 2020 Jan 10.

Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor

Julien Lefranc  1 , Volker Klaus Schulze  1 , Roman Christian Hillig  1 , Hans Briem  1 , Florian Prinz  1 , Anne Mengel  1 , Tobias Heinrich  1 , Jozsef Balint  2 , Srinivasan Rengachari  3 , Horst Irlbacher  1 , Detlef Stöckigt  1 , Ulf Bömer  1 , Benjamin Bader  1 , Stefan Nikolaus Gradl  1 , Carl Friedrich Nising  1 , Franz von Nussbaum  1 , Dominik Mumberg  1 , Daniel Panne  3   4 , Antje Margret Wengner  1
Affiliations

Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor

Julien Lefranc et al. J Med Chem. .

Abstract

The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKKε are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKKε inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.

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