2. Academic Validation
  3. Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5)

Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5)

  • J Med Chem. 2009 Dec 10;52(23):7901-5. doi: 10.1021/jm900807w.
Frederick W Goldberg 1,  Richard A Ward,  Steven J Powell,  Judit E Debreczeni,  Richard A Norman,  Nicola J Roberts,  Allan P Dishington,  Helen J Gingell,  Kate F Wickson,  Andrew L Roberts
Affiliations

Affiliation

  • 1 AstraZeneca, Mereside, Alderley Park, Macclesfield SK10 4TG, UK.
PMID: 19736928 DOI: 10.1021/jm900807w
Abstract

A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor (also known as activin-like kinase 5 or ALK5) inhibitors is reported. The binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel synthetic ideas. Compounds such as 19 are potent ALK5 inhibitors with good physicochemical and pharmacokinetic properties and thus represent high quality leads for further optimization.

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