Document Report Card

ID: ALA1142524

Journal: J Med Chem

Title: Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach.

Authors: Chen X, Wilson LJ, Malaviya R, Argentieri RL, Yang SM.

Abstract: In an effort to identify novel Janus kinase 3 inhibitors, a sequential focused screening approach was adopted to search our in-house chemical database. By biologically testing only 79 selected compounds, we successfully identified 19 compounds showing IC 50 < 20 microM, with four of them in the nanomolar range. Particularly, a 3,5-disubstituted pyrazolo[4,3- d]pyrimidine scaffold emerged as a promising candidate for further lead optimization. With the advantages of efficiency and flexibility, this approach may be utilized to identify leads for other therapeutic targets.

CiteXplore: 18844338

DOI: 10.1021/jm800662z