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Literature summary extracted from

  • Li, X.; Wang, J.; Li, J.; Wu, J.; Li, Y.; Zhu, H.; Fan, R.; Xu, W.
    Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I) (2009), Bioorg. Med. Chem., 17, 3053-3060.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.11.2 (R)-4-(4-carboxy-2-(3,4,5-trimethoxybenzamido)butanamido)-2-hydroxybenzoic acid
-
 Sus scrofa
3.4.11.2 (R)-4-(4-carboxy-2-(3,4,5-trimethoxybenzamido)butanamido)benzoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(2,4-difluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(2,5-dichlorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(2-chloroethylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(2-nicotinoylhydrazinyl)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(3-bromobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(3-chloro-4-fluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(3-iodobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-aminophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-bromo-2-fluorobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-bromophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-chloro-2-fluorobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-chlorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-fluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-(4-nitrophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-oxo-5-(2-(thiazole-2-carbonyl)hydrazinyl)-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-oxo-5-(thiazol-2-ylamino)-4-(3,4,5-trimethoxybenzamido)pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-oxo-5-4-[(1,3-thiazole-2-amino)sulfonyl]phenylamino-4-[(3,4,5-trimethoxybenzamido)]pentanoic acid
-
 Sus scrofa
3.4.11.2 (R)-5-[4-(aminosulfonyl)phenylamino]-5-oxo-4-[(3,4,5-trimethoxybenzamido)]pentanoic acid
-
 Sus scrofa
3.4.11.2 bestatin
-
 Sus scrofa
3.4.11.2 N-(1-(2-aminophenyl)-2,6-dioxopiperidin-3-yl)-3,4,5-trimethoxybenzamide
-
 Sus scrofa

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.11.2 microsome
-
 Sus scrofa
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.11.2 Zn2+ dependent on Sus scrofa

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.11.2 kidney
-
 Sus scrofa
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.11.2 L-Leu-p-nitroanilide + H2O
-
 Sus scrofa L-Leu + p-nitroaniline
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.11.2 aminopeptidase N
-
 Sus scrofa
3.4.11.2 APN
-
 Sus scrofa
3.4.11.2 CD13
-
 Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.11.2 0.0131
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa bestatin
3.4.11.2 0.0234
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-aminophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0243
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-fluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.04
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-chlorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0401
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-oxo-5-4-[(1,3-thiazole-2-amino)sulfonyl]phenylamino-4-[(3,4,5-trimethoxybenzamido)]pentanoic acid
3.4.11.2 0.0419
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-bromophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0456
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-chloro-2-fluorobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0512
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(4-bromo-2-fluorobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0578
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-4-(4-carboxy-2-(3,4,5-trimethoxybenzamido)butanamido)-2-hydroxybenzoic acid
3.4.11.2 0.0658
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-4-(4-carboxy-2-(3,4,5-trimethoxybenzamido)butanamido)benzoic acid
3.4.11.2 0.0659
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(3-iodobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0724
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(2-nicotinoylhydrazinyl)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0785
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(3-chloro-4-fluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0804
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(2,5-dichlorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0877
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-oxo-5-(2-(thiazole-2-carbonyl)hydrazinyl)-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.0896
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(2,4-difluorophenylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.1026
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-[4-(aminosulfonyl)phenylamino]-5-oxo-4-[(3,4,5-trimethoxybenzamido)]pentanoic acid
3.4.11.2 0.104
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa N-(1-(2-aminophenyl)-2,6-dioxopiperidin-3-yl)-3,4,5-trimethoxybenzamide
3.4.11.2 0.1076
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-oxo-5-(thiazol-2-ylamino)-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.1769
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(3-bromobenzylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid
3.4.11.2 0.805
-
 in 50 mM PBS, pH 7.2 at 37°C Sus scrofa (R)-5-(2-chloroethylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido)pentanoic acid