Target Validation Information
TTD ID	T03500
Target Name	Matrix metalloproteinase-12 (MMP-12)
Type of Target	Clinical trial
Drug Potency against Target	(+/-)5-(biphenyl-4-yl)-3-hydroxypentanoic acid	Drug Info	IC50 = 520 nM	[4]
	2-(2-(biphenyl-4-yl)ethylsulfinyl)acetic acid	Drug Info	IC50 = 4500 nM	[4]
	2-(2-(biphenyl-4-yl)ethylsulfonyl)acetic acid	Drug Info	IC50 = 2490 nM	[4]
	2-(2-(biphenyl-4-yl)ethylthio)acetic acid	Drug Info	IC50 = 11800 nM	[4]
	2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide	Drug Info	IC50 = 590 nM	[5]
	3-(4-(2-phenylethynyl)benzoyl)pentanoic acid	Drug Info	IC50 = 480 nM	[2]
	3-(4-Phenylethynylbenzoyl)nonanoic acid	Drug Info	IC50 = 450 nM	[2]
	3-Benzenesulfonyl-heptanoic acid hydroxyamide	Drug Info	IC50 = 9 nM	[1]
	3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide	Drug Info	IC50 = 14 nM	[1]
	4-(4-(dec-1-ynyl)phenyl)-4-oxobutanoic acid	Drug Info	IC50 = 12480 nM	[2]
	5-(3'-cyanobiphenyl-4-yl)-3-hydroxypentanoic acid	Drug Info	IC50 = 3390 nM	[4]
	5-(4'-cyanobiphenyl-4-yl)-3-hydroxypentanoic acid	Drug Info	IC50 = 86 nM	[4]
	5-(biphenyl-4-yl)-3-methoxypentanoic acid	Drug Info	IC50 = 3530 nM	[4]
	5-(biphenyl-4-yl)-3-oxopentanoic acid	Drug Info	IC50 = 7840 nM	[4]
	AGELADINE A	Drug Info	IC50 = 3660 nM	[3]
	GM6001	Drug Info	IC50 = 13 nM	[2]
	N-Hydroxy-2-(4-methoxy-benzenesulfonyl)benzamide	Drug Info	IC50 = 14000 nM	[5]
	N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide	Drug Info	IC50 = 1200 nM	[5]
	[2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid	Drug Info	IC50 = 1500 nM	[5]
References
REF 1	Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. J Med Chem. 2000 Jun 15;43(12):2324-31.
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 of novel ageladine A analogs showing more potent matrix metalloproteinase (MMP)-12 inhibitory activity than the natural product. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5461-3.
REF 4	The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3.
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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