Target Validation Information
TTD ID T68443
Target Name Matrix metalloproteinase-21 (MMP-21)
Type of Target
Literature-reported
Drug Potency against Target 2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info IC50 = 5100 nM [5]
3-(4-(2-phenylethynyl)benzoyl)pentanoic acid Drug Info IC50 = 18070 nM [2]
GM6001 Drug Info IC50 = 17 nM [2]
IK-862 Drug Info Ki = 1599 nM [1]
N-hydroxy-2,3-bis(phenylsulfonamido)propanamide Drug Info Ki = 356 nM [4]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info IC50 = 1300 nM [5]
SR-973 Drug Info Ki = 190 nM [3]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info IC50 = 4300 nM [5]
References
REF 1 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 2 Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids. J Med Chem. 2006 Jan 26;49(2):456-8.
REF 3 Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63.
REF 4 Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3333-7.
REF 5 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.

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