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 530402 | J 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 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 552497 | Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322. | ||||
Ref 525644 | J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. | ||||
Ref 525642 | J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. | ||||
Ref 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 530402 | J 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 526154 | J 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 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 526446 | J 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 525693 | J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects. | ||||
Ref 530402 | J 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 529392 | Bioorg 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 529392 | Bioorg 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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