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Literature summary extracted from

  • Wallen, E.A.; Christiaans, J.A.; Forsberg, M.M.; Venalainen, J.I.; Mannisto, P.T.; Gynther, J.
    Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors (2002), J. Med. Chem., 45, 4581-4584.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.26 3,3-dimethyl glutaric acid bis(L-prolyl-pyrrolidine) amide IC50: 13 nM Sus scrofa
3.4.21.26 adipic acid bis(L-prolyl-pyrrolidine) amide IC50: 68 nM Sus scrofa
3.4.21.26 benzoyl-L-Pro-pyrrolidine IC50: 66 nM Sus scrofa
3.4.21.26 benzyloxycarbonyl-Pro-L-prolinal IC50: 0.33 nM Sus scrofa
3.4.21.26 glutaric acid bis(L-prolyl-pyrrolidine) amide IC50: 48 nM Sus scrofa
3.4.21.26 isophthalic acid bis(L-prolyl-pyrrolidine) amide IC50: 26 nM Sus scrofa
3.4.21.26 isophthalic acid L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine L-prolyl-pyrrolidine amide 0.00039 nM Sus scrofa
3.4.21.26 isophthalic acid L-prolyl-2(S)-cyanopyrrolidine L-prolyl-pyrrolidine amide IC50: 1.5 nM Sus scrofa
3.4.21.26 isophthalic acid L-prolyl-pyrrolidine L-prolyl-L-prolinal amide IC50: 1.3 nM Sus scrofa
3.4.21.26 phthalic acid bis(L-prolyl-pyrrolidine) amide IC50: 0.021 mM Sus scrofa
3.4.21.26 SUAM-1221 IC50: 2.2 nM Sus scrofa
3.4.21.26 succinic acid bis(L-prolyl-pyrrolidine) amide IC50: 77 nM Sus scrofa
3.4.21.26 terephthalic acid bis(L-prolyl-pyrrolidine) amide IC50: 81 nM Sus scrofa

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.26 brain
-
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 0.00000033
-
IC50: 0.33 nM Sus scrofa benzyloxycarbonyl-Pro-L-prolinal
3.4.21.26 0.0000013
-
IC50: 1.3 nM Sus scrofa isophthalic acid L-prolyl-pyrrolidine L-prolyl-L-prolinal amide
3.4.21.26 0.0000015
-
IC50: 1.5 nM Sus scrofa isophthalic acid L-prolyl-2(S)-cyanopyrrolidine L-prolyl-pyrrolidine amide
3.4.21.26 0.0000022
-
IC50: 2.2 nM Sus scrofa SUAM-1221
3.4.21.26 0.000013
-
IC50: 13 nM Sus scrofa 3,3-dimethyl glutaric acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.000026
-
IC50: 26 nM Sus scrofa isophthalic acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.000048
-
IC50: 48 nM Sus scrofa glutaric acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.000066
-
IC50: 66 nM Sus scrofa benzoyl-L-Pro-pyrrolidine
3.4.21.26 0.000068
-
IC50: 68 nM Sus scrofa adipic acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.000077
-
IC50: 77 nM Sus scrofa succinic acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.000081
-
IC50: 81 nM Sus scrofa terephthalic acid bis(L-prolyl-pyrrolidine) amide
3.4.21.26 0.021
-
IC50: 0.021 mM Sus scrofa phthalic acid bis(L-prolyl-pyrrolidine) amide