Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T65019 | ||||
Target Name | Matrix metalloproteinase-14 (MMP-14) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | BMS 275291 | Drug Info | IC50 = 40 nM | [10] | |
2-(4-bromophenylsulfonamido)-N-hydroxyacetamide | Drug Info | IC50 = 360 nM | [8] | ||
2-(biphenyl-4-ylsulfonamido)-N-hydroxyacetamide | Drug Info | IC50 = 70 nM | [8] | ||
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide | Drug Info | IC50 = 8300 nM | [7] | ||
Epigallocatechin gallate | Drug Info | IC50 = 6800 nM | [6] | ||
GM6001 | Drug Info | IC50 = 5.2 nM | [5] | ||
IK-862 | Drug Info | Ki = 15872 nM | [1] | ||
MMI270 | Drug Info | IC50 = 23 nM | [4] | ||
N-hydroxy-2-(4-methoxyphenylsulfonamido)acetamide | Drug Info | IC50 = 210 nM | [8] | ||
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide | Drug Info | IC50 = 1300 nM | [7] | ||
SR-973 | Drug Info | Ki = 1200 nM | [3] | ||
UK-356618 | Drug Info | IC50 = 1900 nM | [2] | ||
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid | Drug Info | IC50 = 5400 nM | [7] | ||
Action against Disease Model | PG-530742 | Drug Info | Selective matrix metalloproteinase inhibition by PG-530742 (at doses 0.2 mg/kg to 3.5 mg/kg) attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure | [9] | |
References | |||||
REF 1 | Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structu... J Med Chem. 2002 Nov 7;45(23):4954-7. | ||||
REF 2 | A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003 Jul 31;46(16):3514-25. | ||||
REF 3 | Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. | ||||
REF 4 | Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. | ||||
REF 5 | Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with i... Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. | ||||
REF 6 | Regioselective synthesis of methylated epigallocatechin gallate via nitrobenzenesulfonyl (Ns) protecting group. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4171-4. | ||||
REF 7 | Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhib... J Med Chem. 2009 Oct 22;52(20):6347-61. | ||||
REF 8 | Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule sheddi... J Med Chem. 2010 Mar 25;53(6):2622-35. | ||||
REF 9 | Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart fail... Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. | ||||
REF 10 | 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. | ||||
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