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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