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

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