Identification of a novel class of autotaxin inhibitors through cross-screening

Diana Castagna, Emma L. Duffy, Dima Semaan, Louise C. Young, John M. Pritchard, Simon J. F. Macdonald, David C. Budd, Craig Jamieson, Allan J. B. Watson

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility.
Original languageEnglish
Pages (from-to)1149-1155
Number of pages7
Issue number6
Publication statusPublished - 1 Jun 2015


  • autotaxin
  • drug discovery
  • lysophosphatidic acid
  • lead compound
  • inhibitor


Dive into the research topics of 'Identification of a novel class of autotaxin inhibitors through cross-screening'. Together they form a unique fingerprint.

Cite this