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  • Richard A. Ward, Paul A. Bethel, +26 authors Baochang Zhai
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 2017 (First Publication: 27 April 2017)
  • There are a number of small-molecule inhibitors targeting the RAS/RAF/MEK/ERK signaling pathway that have either been approved or are in clinical development for oncology across a range of diseaseContinue Reading
  • James J Crawford, Peter W. Kenny, +19 authors Alexander G. Dossetter
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • 2012 (First Publication: 25 October 2012)
  • Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with aContinue Reading
  • Alexander G. Dossetter, Howard H Beeley, +22 authors Madeleine L. Vickers
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • 2012 (First Publication: 26 July 2012)
  • Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reducedContinue Reading
  • Alexander G. Dossetter, Jonathan Bowyer, +17 authors Caroline E. Smith
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2012 (First Publication: 1 September 2012)
  • The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and inhibition ofContinue Reading
  • Chris De Savi, Andrew R. Pape, +11 authors Stefan Gerhardt
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2011 (First Publication: 1 March 2011)
  • Two series of N-hydroxyformamide inhibitors of ADAM-TS4 were identified from screening compounds previously synthesised as inhibitors of matrix metalloproteinase-13 (collagenase-3). Understanding ofContinue Reading
  • Richard A. Ward, Mark J. Anderton, +35 authors Baochang Zhai
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 2019 (First Publication: 11 November 2019)
  • The RAS/MAPK pathway is a major driver of oncogenesis and is dysregulated in approximately 30% of human cancers, primarily by mutations in the BRAF or RAS genes. The extracellular-signal-regulatedContinue Reading