Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameNeutrophil collagenase    
Type of TargetSuccessful target    
Drug Potency against TargetMarimastatIC50 = 2 nM[1]
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamideIC50 = 1000 nM[2]
2-(biphenyl-4-ylsulfonamido)pentanedioic acidIC50 = 1024 nM[3]
3-(4-Methoxy-benzenesulfonyl)-propane-1-thiolIC50 = 1100 nM[4]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic AcidIC50 = 290 nM[2]
BB-1101IC50 = 3 nM[5]
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiolIC50 = 4 nM[4]
CGS-27023AIC50 = 4.4 nM[6]
Ro-37-9790IC50 = 4.9 nM[7]
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiolIC50 = 585 nM[4]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamideIC50 = 620 nM[2]
4-amino-3-(4-(hexyloxy)phenyl)-4-oxobutanoic acidIC50 = 670 nM[3]
Ro-32-3555IC50 = 7 nM[7]
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiolIC50 = 8 nM[4]
SC-44463Ki = 0.7 nM[9]
IK-682Ki = 257 nM[10]
Ref 1Curr Pharm Des. 2005;11(3):295-322.Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. To Reference
Ref 2J 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. To Reference
Ref 3Bioorg 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. To Reference
Ref 4Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. To Reference
Ref 5J Med Chem. 1999 Nov 18;42(23):4890-908.New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. To Reference
Ref 6J Med Chem. 1999 Nov 4;42(22):4547-62.Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. To Reference
Ref 7Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997) To Reference
Ref 8Bioorg. Med. Chem. Lett. 5(4):349-352 (1995) To Reference
Ref 9J 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. To Reference
Ref 10J 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. To Reference
Ref 11J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects. To Reference


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