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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