The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/¦Â-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.

Reference:

Yueshan Li, et al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Feb 10;65(3):1786-1807.  doi: 10.1021/acs.jmedchem.1c00672.