Target Validation Information
Target ID T73475
Target Name Matrilysin
Target Type
Successful
Drug Potency against Target RS-39066 Drug Info IC50 = 0.23 nM
Prinomastat Drug Info Ki = 54 nM [552232]
IK-682 Drug Info Ki = 259 nM [526446]
SR-973 Drug Info Ki = 660 nM [528025]
SC-44463 Drug Info IC50 = 30 nM [526680]
3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide Drug Info IC50 = 290 nM [525813]
Folate gamma-L-phenylalaninehydroxamic acid Drug Info IC50 = 15000 nM [528548]
BB-3644 Drug Info IC50 = 5 nM [552497]
BMS 275291 Drug Info IC50 = 23 nM [552278]
N-hydroxy-2,3-bis(phenylsulfonamido)propanamide Drug Info Ki = 2800 nM [529443]
MMI270 Drug Info IC50 = 100 nM [528548]
Marimastat Drug Info Ki = 16 nM [552892]
3-Benzenesulfonyl-heptanoic acid hydroxyamide Drug Info IC50 = 1200 nM [525813]
References
Ref 552232Mutations in the Plk gene lead to instability of Plk protein in human tumour cell lines. Nat Cell Biol. 2000 Nov;2(11):852-4.
Ref 526446J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Ref 528025Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Ref 526680J Med Chem. 2003 Jul 31;46(16):3514-25.A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.
Ref 525813J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
Ref 528548Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.
Ref 552497Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322.
Ref 552278Inhibition of angiogenesis and metastasis in two murine models by the matrix metalloproteinase inhibitor, BMS-275291. Cancer Res. 2001 Dec 1;61(23):8480-5.
Ref 529443Bioorg Med Chem Lett. 2008 Jun 1;18(11):3333-7. Epub 2008 Apr 16.Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors.
Ref 528548Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.
Ref 552892BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658.
Ref 525813J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.