These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
2 files

Towards a RIOK2 Chemical Probe: Cellular Potency Improvement of a Selective 2-(Acylamino)pyridine Series

submitted on 15.08.2020, 00:35 and posted on 17.08.2020, 12:10 by Christopher Wang, Álvaro Lorente-Macías, Carrow Wells, Julie E. Pickett, Alfredo Picado, William Zuercher, Alison Axtman
RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite research into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl-pyridine based compounds that have both improved cellular activity while maintaining selectivity for RIOK2.


Canada Foundation for Innovation

Eshelman Institute for Innovation

Genome Canada

Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD grant no. 115766]

Ontario Ministry of Economic Development and Innovation

São Paulo Research Foundation-FAPESP

Wellcome [106169/ZZ14/Z]

NC Biotechnology Center Institutional Support Grant 2018-IDG-1030

National Institutes of Health 1U24DK11604

American Foundation for Pharmaceutical Education (AFPE) Foundation

Spanish MECD (FPU 14/00818)


Email Address of Submitting Author


University of North Carolina at Chapel Hill


United States

ORCID For Submitting Author


Declaration of Conflict of Interest

no conflict of interest