2. Academic Validation
  3. Novel Potent Selective Orally Active S1P5 Receptor Antagonists

Novel Potent Selective Orally Active S1P5 Receptor Antagonists

  • ACS Med Chem Lett. 2021 Jan 15;12(3):351-355. doi: 10.1021/acsmedchemlett.0c00631.
Bin Ma 1,  Kevin M Guckian 1,  Xiao-Gao Liu 1,  Chunhua Yang 1,  Bing Li 1,  Robert Scannevin 1,  Michaël Mingueneau 1,  Annabelle Drouillard 2 3,  Thierry Walzer 2 3
Affiliations

Affiliations

  • 1 Medicinal Chemistry, Research, Biogen Inc., 225 Binney St., Cambridge, Massachusetts 02142, United States.
  • 2 Université Lyon 1, Lyon 69007, France.
  • 3 International Center for Infectiology Research, Lyon 69007, France.
PMID: 33738061 DOI: 10.1021/acsmedchemlett.0c00631
Abstract

S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.

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