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

Castagna, Diana and Duffy, Emma L. and Semaan, Dima and Young, Louise C. and Pritchard, John M. and Macdonald, Simon J. F. and Budd, David C. and Jamieson, Craig and Watson, Allan J. B. (2015) Identification of a novel class of autotaxin inhibitors through cross-screening. MedChemComm, 2015 (6). pp. 1149-1155. ISSN 2040-2503 (

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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.


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