Target

Caspase-6 SBDD

Halting the Inflammation Process

  • Activated in human fibrotic conditions and NASH
  • Inhibitors are efficacious in HFD mouse in vivo NASH model
  • Robust BC and cell assays
  • Inhibitors (IC50 = 1-10 nM) of active and inactive forms
    Soluble
    Low CYP liability
    Permeable
    Low hERG liability
    Metabolically stable
    Selective
  • Protein crystal structures solved for both forms
  • SBDD enabled
  • Allosteric inhibition observed
  • Implicated in neurodegeneration

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