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Keywords:

  • biological activity;
  • drug design;
  • enzymes;
  • medicinal chemistry;
  • structural bioinformatics
Thumbnail image of graphical abstract

A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their capabilities to modulate Btk's activity were characterized both in vitro and in vivo. Oral treatment with once-a-day dosing of compound 4 greatly inhibited disease development in a rodent rheumatoid arthritis (RA) model.