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Literature summary for 3.1.1.1 extracted from

  • Williams, E.T.; Jones, K.O.; Ponsler, G.D.; Lowery, S.M.; Perkins, E.J.; Wrighton, S.A.; Ruterbories, K.J.; Kazui, M.; Farid, N.A.
    The biotransformation of prasugrel, a new thienopyridine prodrug, by the human carboxylesterases 1 and 2 (2008), Drug Metab. Dispos., 36, 1227-1232.
    View publication on PubMed
Search for more literature for 3.1.1.1

Inhibitors

Inhibitors Comment Organism Structure
prasugrel inhibits isozyme CE2 at high concentrations in vitro but not in vivo Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00925
-
 2-acetoxy-5-(alpha-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine isozyme CE1 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Caco-2 cell isozyme CE2 Homo sapiens
-
intestine isozyme CE2 Homo sapiens
-
liver isozyme CE1 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-acetoxy-5-(alpha-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine + H2O also called prasugrel, the hydrolysis is at least 25times greater with CE2 than CE1 Homo sapiens 2-[2-oxo-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone + ? also called R-95913 ?
4-nitrophenyl acetate + H2O
-
 Homo sapiens 4-nitrophenol + acetate
-
 ?

Synonyms

Synonyms Comment Organism
CE1 isozyme Homo sapiens
CE2 isozyme Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0765
-
 isozyme CE2 Homo sapiens prasugrel