Target Validation Information
TTD ID T54156
Target Name Matrix metalloproteinase-9 (MMP-9)
Type of Target
Clinical trial
Drug Potency against Target BB-3644 Drug Info IC50 = 70 nM [25]
BMS 275291 Drug Info IC50 = 27 nM [23]
Marimastat Drug Info IC50 = 0.85 nM [24]
PG-530742 Drug Info Complete Inhibition = 150 ng/mL [21]
Prinomastat Drug Info IC50 = 0.26 nM [25]
Tanomastat Drug Info Ki = 301 nM [22]
(+/-)5-(biphenyl-4-yl)-3-hydroxypentanoic acid Drug Info IC50 = 16500 nM [17]
2-(4'-chloro-biphenyl-4-sulfonyl)-pentanoic acid Drug Info IC50 = 10005 nM [10]
2-(biphenyl-4-ylsulfonamido)pentanedioic acid Drug Info IC50 = 14000 nM [13]
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info IC50 = 7700 nM [18]
3-(4-(2-phenylethynyl)benzoyl)pentanoic acid Drug Info IC50 = 3600 nM [8]
3-(4-Phenylethynylbenzoyl)nonanoic acid Drug Info IC50 = 5410 nM [8]
4-amino-3-(4-(hexyloxy)phenyl)-4-oxobutanoic acid Drug Info IC50 = 160 nM [13]
5-(4-Phenoxy-phenyl)-pyrimidine-2,4,6-trione Drug Info IC50 = 14000 nM [3]
5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione Drug Info IC50 = 696 nM [3]
5-Biphenyl-4-yl-5-hexyl-pyrimidine-2,4,6-trione Drug Info IC50 = 863 nM [3]
5-Hexyl-5-phenyl-pyrimidine-2,4,6-trione Drug Info IC50 = 330 nM [3]
5-Methyl-5-phenyl-pyrimidine-2,4,6-trione Drug Info IC50 = 11000 nM [3]
CIPEMASTAT Drug Info Ki = 59 nM [2]
CIPEMASTAT Drug Info IC50 = 59 nM
Curcumin Drug Info IC50 = 8500 nM [16]
GM6001 Drug Info IC50 = 0.6 nM [15]
IK-862 Drug Info Ki = 10340 nM [5]
Methotrexate gamma-L-phenylalaninehydroxamic acid Drug Info IC50 = 15000 nM [11]
MMI270 Drug Info IC50 = 10 nM [1]
N-hydroxy-2,3-bis(phenylsulfonamido)propanamide Drug Info Ki = 227 nM [14]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info IC50 = 690 nM [18]
N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide Drug Info IC50 = 1410 nM [12]
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl) Drug Info IC50 = 5660 nM [12]
RO-319790 Drug Info IC50 = 12 nM [19]
Ro-37-9790 Drug Info IC50 = 10.4 nM
RS-130830 Drug Info Ki = 0.55 nM [7]
SC-44463 Drug Info Ki < 1 nM [4]
SR-973 Drug Info Ki = 5 nM [9]
UK-356618 Drug Info IC50 = 840 nM [6]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info IC50 = 7300 nM [18]
Action against Disease Model Neovastat Drug Info Neovastat prevented the degradation of osteoid-like radiolabeled extracellular matrices which was induced by incubation of h uMan SaOS-2 osteoblast-like cells with MDA-MB-231 cells. Moreover, Neovastat was demonstrated to inhibit the gelatinolytic activity of matrix metalloproteinase (MMP)-9 expressed by MDA-MB-231 cells [20]
References
REF 1 Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors. Bioorg Med Chem Lett. 1999 Jun 21;9(12):1691-6.
REF 2 Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41.
REF 3 Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72.
REF 4 Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivati... J Med Chem. 2001 Oct 11;44(21):3347-50.
REF 5 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 6 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 7 Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6.
REF 8 Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids. J Med Chem. 2006 Jan 26;49(2):456-8.
REF 9 Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63.
REF 10 Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3096-100.
REF 11 Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. Bioorg Med Chem. 2007 Feb 1;15(3):1266-74.
REF 12 Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. Bioorg Med Chem. 2008 Jan 1;16(1):530-5.
REF 13 Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. Bioorg Med Chem. 2009 Feb 1;17(3):1101-8.
REF 14 Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3333-7.
REF 15 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 16 Synthesis and biological evaluation of curcuminoid pyrazoles as new therapeutic agents in inflammatory bowel disease: effect on matrix metalloprote... Bioorg Med Chem. 2009 Feb 1;17(3):1290-6.
REF 17 The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3.
REF 18 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 19 The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8.
REF 20 The effect of Neovastat (AE-941) on an experimental metastatic bone tumor model. Int J Oncol. 2002 Feb;20(2):299-303.
REF 21 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 22 BAY 12-9566, a novel inhibitor of matrix metalloproteinases with antiangiogenic activity. Clin Cancer Res. 1999 Nov;5(11):3603-7.
REF 23 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 24 The evolution of the matrix metalloproteinase inhibitor drug discovery program at abbott laboratories. Curr Top Med Chem. 2004;4(12):1255-67.
REF 25 Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322.

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