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Literature summary for 3.4.11.2 extracted from

  • Li, Q.; Fang, H.; Wang, X.; Xu, W.
    Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II (2010), Eur. J. Med. Chem., 45, 1618-1626.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-amino-N-((S)-1-(2-(hydroxyamino)-2-oxoethyl)-2,6-dioxopiperidin-3-yl)-2-((R)-pyrrolidin-2-yl)acetamide
-
Sus scrofa
bestatin
-
Sus scrofa
ethyl (S)-2-(3-(2-aminoacetamido)-2,6-dioxopiperidin-1-yl)acetate
-
Sus scrofa
ethyl [(3S)-2,6-dioxo-3-(phenylalanylamino)piperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-2,6-dioxo-3-(tryptophylamino)piperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-2,6-dioxo-3-(tyrosylamino)piperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-2,6-dioxo-3-(valylamino)piperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(alanylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(histidylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(isoleucylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(leucylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(lysylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-(methionylamino)-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
ethyl [(3S)-3-{[(2S)-2-amino-2-(pyrrolidin-2-yl)acetyl]amino}-2,6-dioxopiperidin-1-yl]acetate
-
Sus scrofa
N-[(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl]-3,4,5-trimethoxybenzamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}alaninamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}glycinamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}isoleucinamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}leucinamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}lysinamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}phenylalaninamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}tyrosinamide
-
Sus scrofa
N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}valinamide
-
Sus scrofa
[(3S)-2,6-dioxo-3-(phenylalanylamino)piperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-2,6-dioxo-3-(tyrosylamino)piperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-2,6-dioxo-3-(valylamino)piperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-(alanylamino)-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-(glycylamino)-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-(isoleucylamino)-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-(leucylamino)-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-(lysylamino)-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa
[(3S)-3-{[(2S)-2-amino-2-(pyrrolidin-2-yl)acetyl]amino}-2,6-dioxopiperidin-1-yl]acetic acid
-
Sus scrofa

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Sus scrofa
-
-

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Leu-4-nitroanilide + H2O
-
Sus scrofa L-Leu + 4-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
aminopeptidase N
-
Sus scrofa
APN
-
Sus scrofa
CD13
-
Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0018
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}phenylalaninamide
0.0024
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa bestatin
0.0031
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-[(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl]-3,4,5-trimethoxybenzamide
0.0053
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}leucinamide
0.0073
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}tyrosinamide
0.0092
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}isoleucinamide
0.0094
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}glycinamide
0.0094
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}lysinamide
0.0097
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-amino-N-((S)-1-(2-(hydroxyamino)-2-oxoethyl)-2,6-dioxopiperidin-3-yl)-2-((R)-pyrrolidin-2-yl)acetamide
0.0109
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}alaninamide
0.0113
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-2,6-dioxo-3-(tyrosylamino)piperidin-1-yl]acetic acid
0.0125
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa N-{(3S)-1-[2-(hydroxyamino)-2-oxoethyl]-2,6-dioxopiperidin-3-yl}valinamide
0.0132
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-{[(2S)-2-amino-2-(pyrrolidin-2-yl)acetyl]amino}-2,6-dioxopiperidin-1-yl]acetic acid
0.0141
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-(lysylamino)-2,6-dioxopiperidin-1-yl]acetic acid
0.0154
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-(glycylamino)-2,6-dioxopiperidin-1-yl]acetic acid
0.0158
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-2,6-dioxo-3-(valylamino)piperidin-1-yl]acetic acid
0.0166
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-(isoleucylamino)-2,6-dioxopiperidin-1-yl]acetic acid
0.0169
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-2,6-dioxo-3-(tyrosylamino)piperidin-1-yl]acetate
0.0169
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-2,6-dioxo-3-(phenylalanylamino)piperidin-1-yl]acetic acid
0.0189
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(histidylamino)-2,6-dioxopiperidin-1-yl]acetate
0.0207
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-2,6-dioxo-3-(tryptophylamino)piperidin-1-yl]acetate
0.0215
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-(alanylamino)-2,6-dioxopiperidin-1-yl]acetic acid
0.0221
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa [(3S)-3-(leucylamino)-2,6-dioxopiperidin-1-yl]acetic acid
0.0233
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(isoleucylamino)-2,6-dioxopiperidin-1-yl]acetate
0.0237
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl (S)-2-(3-(2-aminoacetamido)-2,6-dioxopiperidin-1-yl)acetate
0.0288
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-2,6-dioxo-3-(valylamino)piperidin-1-yl]acetate
0.0308
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(leucylamino)-2,6-dioxopiperidin-1-yl]acetate
0.0321
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-{[(2S)-2-amino-2-(pyrrolidin-2-yl)acetyl]amino}-2,6-dioxopiperidin-1-yl]acetate
0.0381
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-2,6-dioxo-3-(phenylalanylamino)piperidin-1-yl]acetate
0.041
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(lysylamino)-2,6-dioxopiperidin-1-yl]acetate
0.042
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(methionylamino)-2,6-dioxopiperidin-1-yl]acetate
0.0643
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa ethyl [(3S)-3-(alanylamino)-2,6-dioxopiperidin-1-yl]acetate