Target Validation Information
Target ID T67272
Target Name Aminopeptidase N
Target Type
Clinical Trial
Drug Potency against Target (S)-2-Amino-4-methyl-pentane-1-thiol Drug Info Ki = 22 nM [1]
1-aminobutylphosphonic acid Drug Info IC50 = 15000 nM [2]
Angiotensin IV Drug Info Ki = 830 nM [3]
N1-benzyl-N3-hydroxy-2-isobutylmalonamide Drug Info IC50 = 590 nM [4]
N1-hydroxy-2-isobutyl-N3-phenethylmalonamide Drug Info IC50 = 984 nM [4]
N-Hydroxy-2-(naphthalen-2-ylsulfanyl)-acetamide Drug Info Ki = 3500 nM [5]
KELATORPHAN Drug Info IC50 = 380 nM [6]
N4-Butyl-2-cinnamamido-N1-hydroxysuccinamide Drug Info IC50 = 11100 nM [7]
1-aminohexylphosphonic acid Drug Info IC50 = 8300 nM [2]
(Amino-phenyl-methyl)-phosphinic acid Drug Info Ki = 4800 nM [1]
(S)-2-Amino-4-methylsulfanyl-butane-1-thiol Drug Info Ki = 11 nM [1]
(S)-2-Amino-propane-1-thiol Drug Info Ki = 28 nM [1]
(1-Amino-2-phenyl-ethyl)-phosphinic acid Drug Info Ki = 960 nM [1]
(1-Amino-3-methylsulfanyl-propyl)-phosphinic acid Drug Info Ki = 400 nM [1]
(S)-2-Amino-3-phenyl-propane-1-thiol Drug Info Ki = 30 nM [1]
(1-Amino-3-methyl-butyl)-phosphinic acid Drug Info Ki = 1200 nM [1]
(S)-2-Amino-4-phenyl-butane-1-thiol Drug Info Ki = 27 nM [1]
(S)-2-Amino-2-phenyl-ethanethiol Drug Info Ki = 25 nM [1]
2-Cinnamamido-N4-hexyl-N1-hydroxysuccinamide Drug Info IC50 = 18100 nM [7]
(1-Amino-3-phenyl-propyl)-phosphinic acid Drug Info Ki = 130 nM [1]
2-Cinnamamido-N1-hydroxy-N4-pentylsuccinamide Drug Info IC50 = 17400 nM [7]
2-Cinnamamido-N1-hydroxy-N4-octylsuccinamide Drug Info IC50 = 18500 nM [7]
1-aminohexylphosphonic acid monophenyl ester Drug Info IC50 = 4800 nM [2]
1-aminopentylphosphonic acid monophenyl ester Drug Info IC50 = 5600 nM [2]
(1-Amino-ethyl)-phosphinic acid Drug Info Ki = 8400 nM [1]
References
REF 1Bioorg Med Chem Lett. 1999 Jun 7;9(11):1511-6.Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor.
REF 2Bioorg Med Chem. 2010 Apr 15;18(8):2930-6. Epub 2010 Mar 1.New aromatic monoesters of alpha-aminoaralkylphosphonic acids as inhibitors of aminopeptidase N/CD13.
REF 3Bioorg Med Chem. 2008 Jul 15;16(14):6924-35. Epub 2008 May 27.Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
REF 4Bioorg Med Chem. 2007 Jan 1;15(1):63-76. Epub 2006 Oct 12.A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.
REF 5Bioorg Med Chem Lett. 2005 Jan 3;15(1):181-3.N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
REF 6J Med Chem. 1988 Sep;31(9):1825-31.Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
REF 7Bioorg Med Chem. 2009 Oct 15;17(20):7398-404. Epub 2009 Sep 24.Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13.

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