2. Academic Validation
  3. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors

Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors

  • Bioorg Med Chem Lett. 2016 Sep 1;26(17):4334-9. doi: 10.1016/j.bmcl.2016.07.030.
Haixia Wang 1,  J David Lawson 1,  Nick Scorah 1,  Ruhi Kamran 1,  Mark S Hixon 1,  Joy Atienza 1,  Douglas R Dougan 1,  Mark Sabat 1
Affiliations

Affiliation

  • 1 Takeda California, 10410 Science Center Drive, San Diego, CA 92121, United States.
PMID: 27460209 DOI: 10.1016/j.bmcl.2016.07.030
Abstract

Using SBDD, a series of 4-amino-7-azaindoles were discovered as a novel class of ALK5 inhibitors that are potent in both ALK5 enzymatic and cellular assays. Subsequently a ring cyclization strategy was utilized to improve ADME properties leading to the discovery of a series of 1H-imidazo[4,5-c]pyridin-2(3H)-one drug like ALK5 inhibitors.

Keywords

Activin; Alk5; Factor; Growth; Inhibitors; Kinase; SBDD; Transforming.

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