Target Validation Information
Target ID T61746
Target Name Cathepsin B
Target Type
Discontinued
Drug Potency against Target L-873724 Drug Info IC50 = 925 nM [1]
Ac-hPhe-Leu-Ala-LeuVSMe Drug Info IC50 = 1600 nM [2]
Cbz-Ile-Leu-Ala-LeuVSMe Drug Info IC50 = 5800 nM [2]
Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe Drug Info IC50 = 18000 nM [2]
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe Drug Info Ki = 0.13 nM [3]
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 Drug Info Ki = 13 nM [3]
Z-leu-Val-Agly-Val-OBzl Drug Info Ki = 40 nM [3]
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe Drug Info Ki = 1.41 nM [3]
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl Drug Info Ki = 0.25 nM [3]
Ac-hPhe-Leu-Phe-LeuVSMe Drug Info IC50 = 850 nM [2]
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 Drug Info Ki = 7.29 nM [3]
Z-Ala-Leu-lle-Agly-Ile-Val-OMe Drug Info Ki = 0.3 nM [3]
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe Drug Info Ki = 1.58 nM [3]
L-006235-1 Drug Info IC50 = 17 nM [4]
Gold trichloride sodium chloride Drug Info Ki = 4200 nM [5]
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 Drug Info Ki = 43 nM [3]
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 Drug Info Ki = 0.12 nM [3]
1-(phenyl(p-tolyl)methylene)thiosemicarbazide Drug Info IC50 = 13000 nM [6]
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone Drug Info IC50 = 5690 nM [7]
PTosyl-Glu(OtBu)-Ala-LeuVSMe Drug Info IC50 = 13000 nM [2]
GNF-PF-5434 Drug Info Ki = 64 nM [8]
MDL-2170 Drug Info IC50 = 1360 nM [9]
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone Drug Info IC50 = 9493 nM [10]
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate Drug Info IC50 = 810 nM [11]
References
REF 1Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.The identification of potent, selective, and bioavailable cathepsin S inhibitors.
REF 2J Med Chem. 2006 May 18;49(10):2953-68.Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
REF 3J Med Chem. 2002 Sep 12;45(19):4202-11.Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.
REF 4J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
REF 5Bioorg Med Chem Lett. 2004 Oct 18;14(20):5113-6.Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
REF 6Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
REF 7Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. Epub 2010 Jan 6.Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
REF 8Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells.
REF 9J Med Chem. 2009 May 14;52(9):3093-7.Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
REF 10Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. Epub 2010 Sep 15.Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
REF 11Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?.

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