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
SolubleLow CYP liabilityPermeableLow hERG liabilityMetabolically stableSelective - Protein crystal structures solved for both forms
- SBDD enabled
- Allosteric inhibition observed
- Implicated in neurodegeneration