Small-molecule inhibitor: ONO-6818
Name
- Common name
- ONO-6818
Inhibition
- Peptidases inhibited
- ONO-6818 is an inhibitor of neutrophil elastase (Hirota et al., 2004), and is regarded as a highly specific one.
- Mechanism
- Inhibition is reversible, and has a transition-state mechanism. The structure of an enzyme-inhibitor complex described by Odagaki et al. (2001) shows the electrophilic ketone of the inhibitor covalently bound to O gamma of Ser195 at the active site.
- Pharmaceutical relevance
- Active in experimental models of inflammation (Kuraki et al., 2002; Hirota et al., 2004).
Chemistry
- CID at PubChem
- 4596
- Structure
![[ONO-6818 (S01.131 inhibitor) structure ]](/merops/smi/structures/ono6818.gif)
- Chemical/biochemical name
- 2-(5-amino-6-oxo-2-phenyl-pyrimidin-1-yl)-N-[1-hydroxy-3-methyl-1-(5-tert-butyl-1,3,4-oxadiazol-2-yl)butan-2-yl]acetamide; N-[2-[5-(tert-butyl)-1,3,4-oxadiazol-2-yl]-(IRS)-1-(methylethyl)-2-oxoethyl]-2-(5-amino-6-oxo-2-phenyl-6H-pyrimidin-1-ly)acetamide
- Formula weight
- 455
