Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T61746 | ||||
Target Name | Cathepsin B | ||||
Target Type | Discontinued |
||||
Drug Potency against Target | L-873724 | Drug Info | IC50 = 925 nM | [528921] | |
Ac-hPhe-Leu-Ala-LeuVSMe | Drug Info | IC50 = 1600 nM | [528196] | ||
Cbz-Ile-Leu-Ala-LeuVSMe | Drug Info | IC50 = 5800 nM | [528196] | ||
Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe | Drug Info | IC50 = 18000 nM | [528196] | ||
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe | Drug Info | Ki = 0.13 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 | Drug Info | Ki = 13 nM | [526417] | ||
Z-leu-Val-Agly-Val-OBzl | Drug Info | Ki = 40 nM | [526417] | ||
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe | Drug Info | Ki = 1.41 nM | [526417] | ||
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl | Drug Info | Ki = 0.25 nM | [526417] | ||
Ac-hPhe-Leu-Phe-LeuVSMe | Drug Info | IC50 = 850 nM | [528196] | ||
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 | Drug Info | Ki = 7.29 nM | [526417] | ||
Z-Ala-Leu-lle-Agly-Ile-Val-OMe | Drug Info | Ki = 0.3 nM | [526417] | ||
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe | Drug Info | Ki = 1.58 nM | [526417] | ||
L-006235-1 | Drug Info | IC50 = 17 nM | [527882] | ||
Gold trichloride sodium chloride | Drug Info | Ki = 4200 nM | [527220] | ||
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 | Drug Info | Ki = 43 nM | [526417] | ||
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 | Drug Info | Ki = 0.12 nM | [526417] | ||
1-(phenyl(p-tolyl)methylene)thiosemicarbazide | Drug Info | IC50 = 13000 nM | [529432] | ||
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone | Drug Info | IC50 = 5690 nM | [530644] | ||
PTosyl-Glu(OtBu)-Ala-LeuVSMe | Drug Info | IC50 = 13000 nM | [528196] | ||
GNF-PF-5434 | Drug Info | Ki = 64 nM | [529350] | ||
MDL-2170 | Drug Info | IC50 = 1360 nM | [530104] | ||
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone | Drug Info | IC50 = 9493 nM | [531200] | ||
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate | Drug Info | IC50 = 810 nM | [527872] | ||
References | |||||
Ref 528921 | Bioorg 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 528196 | J 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 528196 | J 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 528196 | J 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 526417 | J 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 526417 | J 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 526417 | J 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 526417 | J 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 526417 | J 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 528196 | J 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 526417 | J 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 526417 | J 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 526417 | J 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 527882 | J 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 527220 | Bioorg 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 526417 | J 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 526417 | J 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 529432 | Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. | ||||
Ref 530644 | Bioorg 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 528196 | J 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 529350 | Bioorg Med Chem. 2009 Feb 1;17(3):1064-70. Epub 2008 Feb 7.Substrate optimization for monitoring cathepsin C activity in live cells. | ||||
Ref 530104 | J 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 531200 | Bioorg 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 527872 | Bioorg 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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