Target Validation Information
Target ID T08856
Target Name Neutrophil collagenase
Target Type
Clinical Trial
Drug Potency against Target 2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info IC50 = 1000 nM [530402]
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol Drug Info IC50 = 585 nM [525535]
3-(4-Methoxy-benzenesulfonyl)-propane-1-thiol Drug Info IC50 = 1100 nM [525535]
Marimastat Drug Info IC50 = 2 nM [552497]
BB-1101 Drug Info IC50 = 3 nM [525644]
MMI270 Drug Info IC50 = 4.4 nM [525642]
CIPEMASTAT Drug Info IC50 = 7 nM
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol Drug Info IC50 = 8 nM [525535]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info IC50 = 290 nM [530402]
SC-44463 Drug Info Ki = 0.7 nM [526154]
ILOMASTAT Drug Info Ki < 1 nM
Ro-37-9790 Drug Info IC50 = 4.9 nM
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol Drug Info IC50 = 4 nM [525535]
IK-682 Drug Info Ki = 257 nM [526446]
CIPEMASTAT Drug Info Ki = 4 nM [525693]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info IC50 = 620 nM [530402]
4-amino-3-(4-(hexyloxy)phenyl)-4-oxobutanoic acid Drug Info IC50 = 670 nM [529392]
2-(biphenyl-4-ylsulfonamido)pentanedioic acid Drug Info IC50 = 1024 nM [529392]
References
Ref 530402J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Ref 525535Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors.
Ref 525535Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors.
Ref 552497Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322.
Ref 525644J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Ref 525642J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Ref 525535Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors.
Ref 530402J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Ref 526154J Med Chem. 2001 Oct 11;44(21):3347-50.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 derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Ref 525535Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors.
Ref 526446J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Ref 525693J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects.
Ref 530402J Med Chem. 2009 Oct 22;52(20):6347-61.Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Ref 529392Bioorg Med Chem. 2009 Feb 1;17(3):1101-8. Epub 2008 Mar 8.Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
Ref 529392Bioorg Med Chem. 2009 Feb 1;17(3):1101-8. Epub 2008 Mar 8.Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.

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