Target Validation Information
Target ID T03500
Target Name MMP-12
Target Type
Clinical Trial
Drug Potency against Target 4-(4-(dec-1-ynyl)phenyl)-4-oxobutanoic acid Drug Info IC50 = 12480 nM [527972]
N-Hydroxy-2-(4-methoxy-benzenesulfonyl)benzamide Drug Info IC50 = 14000 nM [530402]
5-(4'-cyanobiphenyl-4-yl)-3-hydroxypentanoic acid Drug Info IC50 = 86 nM [530333]
2-(2-(biphenyl-4-yl)ethylsulfonyl)acetic acid Drug Info IC50 = 2490 nM [530333]
N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Drug Info IC50 = 1200 nM [530402]
5-(3'-cyanobiphenyl-4-yl)-3-hydroxypentanoic acid Drug Info IC50 = 3390 nM [530333]
3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide Drug Info IC50 = 14 nM [525813]
3-(4-(2-phenylethynyl)benzoyl)pentanoic acid Drug Info IC50 = 480 nM [527972]
3-(4-Phenylethynylbenzoyl)nonanoic acid Drug Info IC50 = 450 nM [527972]
2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Drug Info IC50 = 590 nM [530402]
AGELADINE A Drug Info IC50 = 3660 nM [530304]
2-(2-(biphenyl-4-yl)ethylthio)acetic acid Drug Info IC50 = 11800 nM [530333]
2-(2-(biphenyl-4-yl)ethylsulfinyl)acetic acid Drug Info IC50 = 4500 nM [530333]
5-(biphenyl-4-yl)-3-methoxypentanoic acid Drug Info IC50 = 3530 nM [530333]
5-(biphenyl-4-yl)-3-oxopentanoic acid Drug Info IC50 = 7840 nM [530333]
(+/-)5-(biphenyl-4-yl)-3-hydroxypentanoic acid Drug Info IC50 = 520 nM [530333]
3-Benzenesulfonyl-heptanoic acid hydroxyamide Drug Info IC50 = 9 nM [525813]
[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Drug Info IC50 = 1500 nM [530402]
ILOMASTAT Drug Info IC50 = 13 nM [527972]
The Effect of Target Knockout, Knockdown or Genetic Variations Reduced respiratory failure and lung enlargement induced by IL13; Resistance against cigarette-smoke-induced emphysema; Reduced acute lung injury by immune complexes; No protection against TNF-induced hepatitis; Increased maximal EAE severity; Improved functional recovery from spinal cord compression; Spontaneous deficient myelination of corpus callos uM, fewer oligodendrocytes; Retarded in vitro differentiation of oligodendrocytes [527972]
References
Ref 527972J Med Chem. 2006 Jan 26;49(2):456-8.Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
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 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 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 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 525813J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
Ref 527972J Med Chem. 2006 Jan 26;49(2):456-8.Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
Ref 527972J Med Chem. 2006 Jan 26;49(2):456-8.Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
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 530304Bioorg Med Chem Lett. 2009 Sep 15;19(18):5461-3. Epub 2009 Jul 23.Synthesis of novel ageladine A analogs showing more potent matrix metalloproteinase (MMP)-12 inhibitory activity than the natural product.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 530333Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. Epub 2009 Aug 6.The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Ref 525813J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
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 527972J Med Chem. 2006 Jan 26;49(2):456-8.Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.

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