Target Validation Information
TTD ID T08856
Target Name Matrix metalloproteinase-8 (MMP-8)
Type of Target
Clinical trial
Drug Potency against Target Marimastat Drug Info IC50 = 2 nM [9]
2-(biphenyl-4-ylsulfonamido)pentanedioic acid Drug Info IC50 = 1024 nM [7]
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info IC50 = 1000 nM [8]
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol Drug Info IC50 = 585 nM [1]
3-(4-Methoxy-benzenesulfonyl)-propane-1-thiol Drug Info IC50 = 1100 nM [1]
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol Drug Info IC50 = 8 nM [1]
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol Drug Info IC50 = 4 nM [1]
4-amino-3-(4-(hexyloxy)phenyl)-4-oxobutanoic acid Drug Info IC50 = 670 nM [7]
BB-1101 Drug Info IC50 = 3 nM [3]
CIPEMASTAT Drug Info IC50 = 7 nM
CIPEMASTAT Drug Info Ki = 4 nM [4]
GM6001 Drug Info Ki < 1 nM
IK-862 Drug Info Ki = 257 nM [6]
MMI270 Drug Info IC50 = 4.4 nM [2]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info IC50 = 620 nM [8]
Ro-37-9790 Drug Info IC50 = 4.9 nM
SC-44463 Drug Info Ki = 0.7 nM [5]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info IC50 = 290 nM [8]
References
REF 1 Synthesis and identification of conformationally constrained selective MMP inhibitors. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.
REF 2 Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. J Med Chem. 1999 Nov 4;42(22):4547-62.
REF 3 New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. J Med Chem. 1999 Nov 18;42(23):4890-908.
REF 4 Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41.
REF 5 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 6 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 7 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 8 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 9 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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