Target Validation Information
TTD ID	T82393
Target Name	TNF alpha converting enzyme (ADAM17)
Type of Target	Clinical trial
Drug Potency against Target	DPC-333	Drug Info	IC50 = 17~100 nM	[8]
	2-(4-bromophenylsulfonamido)-N-hydroxyacetamide	Drug Info	IC50 = 3900 nM	[7]
	2-(biphenyl-4-ylsulfonamido)-N-hydroxyacetamide	Drug Info	IC50 = 2400 nM	[7]
	Apratastat	Drug Info	IC50 = 140 nM	[1]
	CIPEMASTAT	Drug Info	Ki = 230 nM	[3]
	IK-862	Drug Info	Ki = 0.56 nM	[5]
	N-hydroxy-2-(4-methoxyphenylsulfonamido)acetamide	Drug Info	IC50 = 1800 nM	[7]
	N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide	Drug Info	IC50 = 150 nM	[4]
	N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl)	Drug Info	IC50 = 110 nM	[4]
	PKF-241-466	Drug Info	IC50 = 141 nM	[6]
	PKF-242-484	Drug Info	IC50 = 56 nM	[6]
	SR-973	Drug Info	Ki = 4 nM	[2]
References
REF 1	Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9.
REF 2	Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63.
REF 3	A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6.
REF 4	Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. Bioorg Med Chem. 2008 Jan 1;16(1):530-5.
REF 5	Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. Bioorg Med Chem. 2008 Oct 1;16(19):8781-94.
REF 6	Current perspective of TACE inhibitors: a review. Bioorg Med Chem. 2009 Jan 15;17(2):444-59.
REF 7	Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule sheddi... J Med Chem. 2010 Mar 25;53(6):2622-35.
REF 8	Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard... J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62.

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