| 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 | [1] | ||
| IK-682 | Drug Info | Ki = 259 nM | [2] | ||
| SR-973 | Drug Info | Ki = 660 nM | [3] | ||
| SC-44463 | Drug Info | IC50 = 30 nM | [4] | ||
| 3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 290 nM | [5] | ||
| Folate gamma-L-phenylalaninehydroxamic acid | Drug Info | IC50 = 15000 nM | [6] | ||
| BB-3644 | Drug Info | IC50 = 5 nM | [7] | ||
| BMS 275291 | Drug Info | IC50 = 23 nM | [8] | ||
| N-hydroxy-2,3-bis(phenylsulfonamido)propanamide | Drug Info | Ki = 2800 nM | [9] | ||
| MMI270 | Drug Info | IC50 = 100 nM | [6] | ||
| Marimastat | Drug Info | Ki = 16 nM | [10] | ||
| 3-Benzenesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 1200 nM | [5] | ||
| References | |||||
| REF 1 | Mutations 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 2 | J 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 3 | Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. | ||||
| REF 4 | J 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 5 | J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. | ||||
| REF 6 | Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. Epub 2006 Nov 14.Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. | ||||
| REF 7 | Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322. | ||||
| REF 8 | Inhibition 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 9 | Bioorg Med Chem Lett. 2008 Jun 1;18(11):3333-7. Epub 2008 Apr 16.Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors. | ||||
| REF 10 | BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658. | ||||
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