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Literature summary for 3.4.21.26 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

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

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Sus scrofa
-

Substrates and Products (Substrate)

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

IC50 Value

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