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Literature summary extracted from

  • Wallen, E.A.; Christiaans, J.A.; Saario, S.M.; Forsberg, M.M.; Venalainen, J.I.; Paso, H.M.; Mannisto, P.T.; Gynther, J.
    4-Phenylbutanoyl-2(S)-acylpyrrolidines and 4-phenylbutanoyl-L-prolyl-2(S)-acylpyrrolidines as prolyl oligopeptidase inhibitors (2002), Bioorg. Med. Chem., 10, 2199-2206.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.26 4-phenylbutanoyl-2(S)-(2-oxocyclopentanecarbonyl)-pyrrolidine IC50: 260 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-(3-phenylpropionyl)pyrrolidine IC50: 0.024 mM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-(cyclohexanecarbonyl)pyrrolidine IC50: 1100 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-(cyclopentanecarbonyl)pyrrolidine IC50: 30 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-(phenylacetyl)pyrrolidine IC50: 3600 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-benzylpyrrolidine IC50: 23 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-2(S)-isobutanoylpyrrolidine IC50: 620 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-L-prolyl-2(S)-(cyclopentanecarbonyl)-pyrrolidine IC%0: 1010 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine IC50: 0.2 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-L-prolyl-2(S)-acetylpyrrolidine IC50: 170 nM Sus scrofa
3.4.21.26 4-phenylbutanoyl-L-prolyl-2(S)-benzoylpyrrolidine IC50: 210 nM Sus scrofa
3.4.21.26 benzyloxycarbonyl-L-Pro-L-prolinal IC50: 0.4 nM Sus scrofa
3.4.21.26 JTP-4819 IC50: 0.2 nM Sus scrofa
3.4.21.26 SUAM-1221 IC50: 2 nM Sus scrofa

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.26 Sus scrofa
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.26 succinyl-Gly-Pro-4-methylcoumaryl-7-amide + H2O
-
 Sus scrofa succinyl-Gly-Pro + 7-amino-4-methylcoumarin
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.26 0.0000002
-
 IC50: 0.2 nM Sus scrofa JTP-4819
3.4.21.26 0.0000002
-
 IC50: 0.2 nM Sus scrofa 4-phenylbutanoyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine
3.4.21.26 0.0000004
-
 IC50: 0.4 nM Sus scrofa benzyloxycarbonyl-L-Pro-L-prolinal
3.4.21.26 0.000002
-
 IC50: 2 nM Sus scrofa SUAM-1221
3.4.21.26 0.000023
-
 IC50: 23 nM Sus scrofa 4-phenylbutanoyl-2(S)-benzylpyrrolidine
3.4.21.26 0.00003
-
 IC50: 30 nM Sus scrofa 4-phenylbutanoyl-2(S)-(cyclopentanecarbonyl)pyrrolidine
3.4.21.26 0.00017
-
 IC50: 170 nM Sus scrofa 4-phenylbutanoyl-L-prolyl-2(S)-acetylpyrrolidine
3.4.21.26 0.00021
-
 IC50: 210 nM Sus scrofa 4-phenylbutanoyl-L-prolyl-2(S)-benzoylpyrrolidine
3.4.21.26 0.00026
-
 IC50: 260 nM Sus scrofa 4-phenylbutanoyl-2(S)-(2-oxocyclopentanecarbonyl)-pyrrolidine
3.4.21.26 0.00062
-
 IC50: 620 nM Sus scrofa 4-phenylbutanoyl-2(S)-isobutanoylpyrrolidine
3.4.21.26 0.0011
-
 IC50: 1100 nM Sus scrofa 4-phenylbutanoyl-2(S)-(cyclohexanecarbonyl)pyrrolidine
3.4.21.26 0.0036
-
 IC50: 3600 nM Sus scrofa 4-phenylbutanoyl-2(S)-(phenylacetyl)pyrrolidine
3.4.21.26 0.024
-
 IC50: 0.024 mM Sus scrofa 4-phenylbutanoyl-2(S)-(3-phenylpropionyl)pyrrolidine