2. Academic Validation
  3. Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors

Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors

  • J Med Chem. 2007 Mar 22;50(6):1280-7. doi: 10.1021/jm061381f.
Alex M Aronov 1,  Christopher Baker,  Guy W Bemis,  Jingrong Cao,  Guanjing Chen,  Pamella J Ford,  Ursula A Germann,  Jeremy Green,  Michael R Hale,  Marc Jacobs,  James W Janetka,  Francois Maltais,  Gabriel Martinez-Botella,  Mark N Namchuk,  Judy Straub,  Qing Tang,  Xiaoling Xie
Affiliations

Affiliation

  • 1 Vertex Pharmaceuticals Inc., 130 Waverly Street, Cambridge, Massachusetts 02139-4242, USA. [email protected]
PMID: 17300186 DOI: 10.1021/jm061381f
Abstract

The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-121280
    ERK2 Inhibitor
    ERK