2. Academic Validation
  3. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor

  • Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. doi: 10.1016/j.bmcl.2011.12.027.
Véronique Plantevin Krenitsky 1,  Lisa Nadolny,  Mercedes Delgado,  Leticia Ayala,  Steven S Clareen,  Robert Hilgraf,  Ronald Albers,  Sayee Hegde,  Neil D'Sidocky,  John Sapienza,  Jonathan Wright,  Meg McCarrick,  Sogole Bahmanyar,  Philip Chamberlain,  Silvia L Delker,  Jeff Muir,  David Giegel,  Li Xu,  Maria Celeridad,  Jeff Lachowitzer,  Brydon Bennett,  Mehran Moghaddam,  Oleg Khatsenko,  Jason Katz,  Rachel Fan,  April Bai,  Yang Tang,  Michael A Shirley,  Brent Benish,  Tracey Bodine,  Kate Blease,  Heather Raymon,  Brian E Cathers,  Yoshitaka Satoh
Affiliations

Affiliation

  • 1 Celgene Corporation, 4550 Towne Centre Court, San Diego, CA 92121, USA. [email protected]
PMID: 22244937 DOI: 10.1016/j.bmcl.2011.12.027
Abstract

In this Letter we describe the discovery of potent, selective, and orally active aminopurine JNK inhibitors. Improving the physico-chemical properties as well as increasing the potency and selectivity of a subseries with rat plasma exposure, led to the identification of four structurally diverse inhibitors. Differentiation based on PK profiles in multiple species as well as activity in a chronic efficacy model led to the identification of 1 (CC-930) as a development candidate, which is currently in Phase II clinical trial for IPF.

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