Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.26 extracted from

  • Wallen, E.A.; Christiaans, J.A.; Saarinen, T.J.; Jarho, E.M.; Forsberg, M.M.; Venalainen, J.I.; Mannisto, P.T.; Gynther, J.
    Conformationally rigid N-acyl-5-alkyl-L-prolyl-pyrrolidines as prolyl oligopeptidase inhibitors (2003), Bioorg. Med. Chem., 11, 3611-3619.
    View publication on PubMed
Search for more literature for 3.4.21.26

Inhibitors

Inhibitors Comment Organism Structure
3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-5(R)-tert-butyl-L-Pro-pyrrolidine IC50: 460 nM Sus scrofa
3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-L-Pro-pyrrolidine IC50: 18 nM Sus scrofa
4-phenylbutanoyl-5(R)-methyl-L-Pro-2(S)-(hydroxyacetyl)pyrrolidine IC50: 0.15 nM Sus scrofa
4-phenylbutanoyl-5(R)-methyl-L-Pro-pyrrolidine IC50: 0.71 nM Sus scrofa
4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine IC50: 0.26 nM Sus scrofa
4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-pyrrolidine IC50: 1.2 nM Sus scrofa
4-phenylbutanoyl-5(S)-methyl-L-Pro-pyrrolidine IC50: 1.4 nM Sus scrofa
4-phenylbutanoyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine IC50: 0.24 nM Sus scrofa
4-phenylbutanoyl-L-Pro-pyrrolidine IC50: 2.2 nM Sus scrofa
acetyl-5(R)-tert-butyl-L-Pro-pyrrolidine IC50: 7100 nM Sus scrofa
benzylcarbamoyl-5(R)-tert-butyl-L-prolyl-pyrrolidine IC50: 2.0 nM Sus scrofa
Boc-5(R)-tert-butyl-L-Pro-pyrrolidine IC50: 2.2 nM Sus scrofa
Boc-5(S)-tert-butyl-L-Pro-pyrrolidine IC50: 9.2 nM Sus scrofa
Boc-L-Pro-pyrrolidine IC50: 29 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
-
 ?

Synonyms

Synonyms Comment Organism
POP
-
 Sus scrofa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000015
-
 4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine pH 7.0, 30°C Sus scrofa
0.000000018
-
 4-phenylbutanoyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine pH 7.0, 30°C Sus scrofa
0.000000026
-
 4-phenylbutanoyl-5(R)-methyl-L-Pro-2(S)-(hydroxyacetyl)pyrrolidine pH 7.0, 30°C Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000015
-
 IC50: 0.15 nM Sus scrofa 4-phenylbutanoyl-5(R)-methyl-L-Pro-2(S)-(hydroxyacetyl)pyrrolidine
0.00000024
-
 IC50: 0.24 nM Sus scrofa 4-phenylbutanoyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine
0.00000026
-
 IC50: 0.26 nM Sus scrofa 4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine
0.00000071
-
 IC50: 0.71 nM Sus scrofa 4-phenylbutanoyl-5(R)-methyl-L-Pro-pyrrolidine
0.0000012
-
 IC50: 1.2 nM Sus scrofa 4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-pyrrolidine
0.0000014
-
 IC50: 1.4 nM Sus scrofa 4-phenylbutanoyl-5(S)-methyl-L-Pro-pyrrolidine
0.000002
-
 IC50: 2.0 nM Sus scrofa benzylcarbamoyl-5(R)-tert-butyl-L-prolyl-pyrrolidine
0.0000022
-
 IC50: 2.2 nM Sus scrofa Boc-5(R)-tert-butyl-L-Pro-pyrrolidine
0.0000022
-
 IC50: 2.2 nM Sus scrofa 4-phenylbutanoyl-L-Pro-pyrrolidine
0.0000092
-
 IC50: 9.2 nM Sus scrofa Boc-5(S)-tert-butyl-L-Pro-pyrrolidine
0.000018
-
 IC50: 18 nM Sus scrofa 3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-L-Pro-pyrrolidine
0.000029
-
 IC50: 29 nM Sus scrofa Boc-L-Pro-pyrrolidine
0.00046
-
 IC50: 460 nM Sus scrofa 3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-5(R)-tert-butyl-L-Pro-pyrrolidine
0.0071
-
 IC50: 7100 nM Sus scrofa acetyl-5(R)-tert-butyl-L-Pro-pyrrolidine