Target Validation Information
Target ID T40332
Target Name Leukocyte elastase
Target Type
Clinical Trial
Drug Potency against Target WIN-63395 Drug Info Ki = 0.27 nM
ZK-814048 Drug Info Ki = 10000 nM [1]
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info Ki = 45 nM [2]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Drug Info Ki = 39 nM [2]
Sivelestat sodium hydrate Drug Info IC50 = 44 nM [3]
FR-901451 Drug Info Ki = 10 nM [4]
FR-901277 Drug Info Ki = 12 nM [4]
4-Hydroxy-3-nonanoyl-6-octyl-pyran-2-one Drug Info Ki = 4600 nM [5]
3-Benzyl-3-ethyl-1-phenylazetidine-2,4-dione Drug Info Ki = 127 nM [6]
Cbz-Val-Pro-Val-(2-benzoxazole) Drug Info Ki = 3 nM [7]
E-6-O-p-methoxycinnamoyl scandoside methyl ester Drug Info IC50 = 18000 nM [8]
EPIGALOCATECHIN GALLATE Drug Info IC50 = 12800 nM [8]
(4-nitro-1H-pyrazol-1-yl)(phenyl)methanone Drug Info Ki = 34 nM [2]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info Ki = 28 nM [2]
(4-bromo-1H-pyrazol-1-yl)(m-tolyl)methanone Drug Info Ki = 250 nM [2]
(4-nitro-1H-pyrazol-1-yl)(o-tolyl)methanone Drug Info Ki = 65 nM [2]
Ac-Ala-Pro-Val-(2-benzoxazole) Drug Info Ki = 73 nM [7]
6-Heptyl-4-hydroxy-3-octanoyl-pyran-2-one Drug Info Ki = 15000 nM [5]
Delanzomib Drug Info IC50 = 3550 nM [9]
4-methoxy-N'-(2-phenylacetyl)benzohydrazide Drug Info Ki = 2500 nM [2]
(4-chloro-1H-pyrazol-1-yl)(o-tolyl)methanone Drug Info Ki = 230 nM [2]
3-butyl-3-ethyl-1-phenylazetidine-2,4-dione Drug Info Ki = 0.85 nM [6]
3,3-Diethyl-1-o-tolylazetidine-2,4-dione Drug Info Ki = 233 nM [6]
3-Benzyl-3-methyl-1-phenylazetidine-2,4-dione Drug Info Ki = 4450 nM [6]
2-methylbut-3-yn-2-yl 4-methoxybenzoate Drug Info Ki = 110 nM [2]
(1H-pyrazol-1-yl)(o-tolyl)methanone Drug Info Ki = 3400 nM [2]
3,3-Diethyl-1-(pyridin-3-yl)azetidine-2,4-dione Drug Info Ki = 2.2 nM [6]
1-benzyl-3,3-diethylazetidine-2,4-dione Drug Info Ki = 114 nM [6]
1-benzyl-3,3-dimethylazetidine-2,4-dione Drug Info Ki = 34.4 nM [6]
N,N-bis(cyanomethyl)-3,4-dimethoxybenzamide Drug Info Ki = 290 nM [2]
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone Drug Info Ki = 46 nM [2]
(3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Drug Info Ki = 104 nM [2]
3-Ethyl-3-isobutyl-1-phenylazetidine-2,4-dione Drug Info Ki = 3.9 nM [6]
3,4-dichloroisocoumarin Drug Info IC50 = 3000 nM [10]
Bornyl (3,4,5-trihydroxy)-cinnamate Drug Info IC50 = 540 nM [11]
3,3-diethyl-1-phenylazetidine-2,4-dione Drug Info Ki = 1.21 nM [6]
3-Decanoyl-4-hydroxy-6-nonyl-pyran-2-one Drug Info Ki = 7900 nM [5]
(4-bromo-1H-pyrazol-1-yl)(o-tolyl)methanone Drug Info Ki = 300 nM [2]
References
REF 1J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors.
REF 2J Med Chem. 2007 Oct 4;50(20):4928-38. Epub 2007 Sep 12.N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.
REF 3Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
REF 4Bioorg Med Chem. 2007 Jul 1;15(13):4618-28. Epub 2007 Apr 3.Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.
REF 5J Med Chem. 1987 Jun;30(6):1017-23.Inhibition of human sputum elastase by substituted 2-pyrones.
REF 6J Med Chem. 2010 Jan 14;53(1):241-53.4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.
REF 7Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. Epub 2007 Nov 6.Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
REF 8Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5. Epub 2009 Nov 26.Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.
REF 9J Med Chem. 2008 Feb 28;51(4):1068-72. Epub 2008 Feb 5.Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
REF 10Antimicrob Agents Chemother. 2007 Feb;51(2):543-50. Epub 2006 Dec 4.Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
REF 11Bioorg Med Chem. 2008 Mar 1;16(5):2385-90. Epub 2007 Nov 29.Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.

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