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 | [525524] | |
1-aminobutylphosphonic acid | Drug Info | IC50 = 15000 nM | [530815] | ||
Angiotensin IV | Drug Info | Ki = 830 nM | [529535] | ||
N1-benzyl-N3-hydroxy-2-isobutylmalonamide | Drug Info | IC50 = 590 nM | [528501] | ||
N1-hydroxy-2-isobutyl-N3-phenethylmalonamide | Drug Info | IC50 = 984 nM | [528501] | ||
N-Hydroxy-2-(naphthalen-2-ylsulfanyl)-acetamide | Drug Info | Ki = 3500 nM | [527322] | ||
KELATORPHAN | Drug Info | IC50 = 380 nM | [533380] | ||
N4-Butyl-2-cinnamamido-N1-hydroxysuccinamide | Drug Info | IC50 = 11100 nM | [530409] | ||
1-aminohexylphosphonic acid | Drug Info | IC50 = 8300 nM | [530815] | ||
(Amino-phenyl-methyl)-phosphinic acid | Drug Info | Ki = 4800 nM | [525524] | ||
(S)-2-Amino-4-methylsulfanyl-butane-1-thiol | Drug Info | Ki = 11 nM | [525524] | ||
(S)-2-Amino-propane-1-thiol | Drug Info | Ki = 28 nM | [525524] | ||
(1-Amino-2-phenyl-ethyl)-phosphinic acid | Drug Info | Ki = 960 nM | [525524] | ||
(1-Amino-3-methylsulfanyl-propyl)-phosphinic acid | Drug Info | Ki = 400 nM | [525524] | ||
(S)-2-Amino-3-phenyl-propane-1-thiol | Drug Info | Ki = 30 nM | [525524] | ||
(1-Amino-3-methyl-butyl)-phosphinic acid | Drug Info | Ki = 1200 nM | [525524] | ||
(S)-2-Amino-4-phenyl-butane-1-thiol | Drug Info | Ki = 27 nM | [525524] | ||
(S)-2-Amino-2-phenyl-ethanethiol | Drug Info | Ki = 25 nM | [525524] | ||
2-Cinnamamido-N4-hexyl-N1-hydroxysuccinamide | Drug Info | IC50 = 18100 nM | [530409] | ||
(1-Amino-3-phenyl-propyl)-phosphinic acid | Drug Info | Ki = 130 nM | [525524] | ||
2-Cinnamamido-N1-hydroxy-N4-pentylsuccinamide | Drug Info | IC50 = 17400 nM | [530409] | ||
2-Cinnamamido-N1-hydroxy-N4-octylsuccinamide | Drug Info | IC50 = 18500 nM | [530409] | ||
1-aminohexylphosphonic acid monophenyl ester | Drug Info | IC50 = 4800 nM | [530815] | ||
1-aminopentylphosphonic acid monophenyl ester | Drug Info | IC50 = 5600 nM | [530815] | ||
(1-Amino-ethyl)-phosphinic acid | Drug Info | Ki = 8400 nM | [525524] | ||
References | |||||
Ref 525524 | Bioorg 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 530815 | Bioorg 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 529535 | Bioorg 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 528501 | Bioorg 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 528501 | Bioorg 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 527322 | Bioorg 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 533380 | J Med Chem. 1988 Sep;31(9):1825-31.Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes. | ||||
Ref 530409 | Bioorg 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. | ||||
Ref 530815 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 525524 | Bioorg 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 530409 | Bioorg 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. | ||||
Ref 525524 | Bioorg 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 530409 | Bioorg 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. | ||||
Ref 530409 | Bioorg 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. | ||||
Ref 530815 | Bioorg 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 530815 | Bioorg 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 525524 | Bioorg 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. |
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