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Literature summary for 3.4.11.2 extracted from

  • Yang, K.; Wang, Q.; Su, L.; Fang, H.; Wang, X.; Gong, J.; Wang, B.; Xu, W.
    Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors (2009), Bioorg. Med. Chem., 17, 3810-3817.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-pentylpropanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-phenethylpropanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-propylpropanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)propanoic acid moderate APN inhibition Sus scrofa
(2R,3S)-2-amino-3-hydroxy-N-((S)-1-(hydroxyamino)-1-oxo-3-phenylpropan-2-yl)-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-N-(4-hydroxyphenethyl)-3-(4-nitrophenyl) propanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-N-(4-methoxybenzyl)-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-3-hydroxy-N-isopropyl-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-N-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-N-(2-chlorophenethyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-N-(4-fluorobenzyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-N-butyl-3-hydroxy-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(2R,3S)-2-amino-N-cyclohexyl-3-hydroxy-3-(4-nitrophenyl)propanamide
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-(1H-indol-2-yl)propanoic acid
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-methylbutanoic acid
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-methylpentanoic acid
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-phenylpropanoic acid
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-4-methylpentanoic acid
-
Sus scrofa
(S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-N-hydroxy-4-methylpentanamide
-
Sus scrofa
(S)-2-((S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-phenylpropanamido)-3-phenylpropanoic acid
-
Sus scrofa
(S)-2-((S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-4-methylpentanamido)-3-phenylpropanoic acid
-
Sus scrofa
4-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)butanoic acid
-
Sus scrofa
6-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)hexanoic acid
-
Sus scrofa
bestatin
-
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
0.003
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa bestatin
0.0071
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-phenylpropanamido)-3-phenylpropanoic acid
0.0313
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-N-((S)-1-(hydroxyamino)-1-oxo-3-phenylpropan-2-yl)-3-(4-nitrophenyl)propanamide
0.0346
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-4-methylpentanamido)-3-phenylpropanoic acid
0.0514
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-N-(4-hydroxyphenethyl)-3-(4-nitrophenyl) propanamide
0.054
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-N-hydroxy-4-methylpentanamide
0.0604
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-phenylpropanoic acid
0.0856
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-4-methylpentanoic acid
0.0903
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-N-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
0.1028
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-methylpentanoic acid
0.1063
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-phenethylpropanamide
0.1163
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-3-(4-nitrophenyl)propanamide
0.1368
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-N-(2-chlorophenethyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
0.1402
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)propanoic acid
0.1447
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-N-(4-methoxybenzyl)-3-(4-nitrophenyl)propanamide
0.1599
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-methylbutanoic acid
0.1622
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (S)-2-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)-3-(1H-indol-2-yl)propanoic acid
0.1699
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-propylpropanamide
0.1832
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-propylpropanamide
0.2326
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-N-butyl-3-hydroxy-3-(4-nitrophenyl)propanamide
0.2507
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-N-isopropyl-3-(4-nitrophenyl)propanamide
0.2513
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-N-cyclohexyl-3-hydroxy-3-(4-nitrophenyl)propanamide
0.3025
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-N-(4-fluorobenzyl)-3-hydroxy-3-(4-nitrophenyl)propanamide
0.5217
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa (2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-N-pentylpropanamide
1.389
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa 6-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)hexanoic acid
2.891
-
in 50 mM PBS buffer, pH 7.2, at 37°C Sus scrofa 4-((2R,3S)-2-amino-3-hydroxy-3-(4-nitrophenyl)-propanamido)butanoic acid