Discovery of BAY-985, a highly selective TBK1/IKK epsilon inhibitor.

Lefranc, J.; Schulze, V. K.; Hillig, R. C.; Briem, H.; Prinz, F.; Mengel, A.; Heinrich, T.; Balint, J.; Rengachari, S.; Irlbacher, H.; Stockigt, D.; Bömer, U.; Bader, B.; Gradl, S. N.; Nising, C. F.; von Nussbaum, F.; Mumberg, D.; Panne, D.; Wengner, A. M.

doi:10.1021/acs.jmedchem.9b01460

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Discovery of BAY-985, a highly selective TBK1/IKK epsilon inhibitor.

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Rengachari, S.
Department of Molecular Biology, MPI for Biophysical Chemistry, Max Planck Society;

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Citation

Lefranc, J., Schulze, V. K., Hillig, R. C., Briem, H., Prinz, F., Mengel, A., et al. (2020). Discovery of BAY-985, a highly selective TBK1/IKK epsilon inhibitor. Journal of Medicinal Chemistry, 63(2), 601-612. doi:10.1021/acs.jmedchem.9b01460.

Cite as: https://hdl.handle.net/21.11116/0000-0005-9B80-B

Abstract

The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKK epsilon are noncanonical members of the inhibitor of the nuclear factor kappa B (I kappa B) 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/IKK epsilon 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.