Target Validation Information
Target ID T82393
Target Name ADAM 17
Target Type
Clinical Trial
Drug Potency against Target N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide Drug Info IC50 = 150 nM [529102]
PKF-241-466 Drug Info IC50 = 141 nM [529876]
SR-973 Drug Info Ki = 4 nM [528025]
PKF-242-484 Drug Info IC50 = 56 nM [529876]
DPC-333 Drug Info IC50 = 17~100 nM [534251]
TMI-05 Drug Info IC50 = 140 nM [527982]
IK-682 Drug Info Ki = 0.56 nM [529692]
CIPEMASTAT Drug Info Ki = 230 nM [528065]
N-hydroxy-2-(4-methoxyphenylsulfonamido)acetamide Drug Info IC50 = 1800 nM [530746]
N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl) Drug Info IC50 = 110 nM [529102]
2-(4-bromophenylsulfonamido)-N-hydroxyacetamide Drug Info IC50 = 3900 nM [530746]
2-(biphenyl-4-ylsulfonamido)-N-hydroxyacetamide Drug Info IC50 = 2400 nM [530746]
References
Ref 529102Bioorg Med Chem. 2008 Jan 1;16(1):530-5. Epub 2007 Sep 14.Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.
Ref 529876Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review.
Ref 528025Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Ref 529876Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review.
Ref 534251J Pharmacol Toxicol Methods. 1996 Sep;36(1):53-62.Characterization of [3H]apafant binding to PAF receptor on rabbit platelet membranes: a comparison of a microplate filtration system and a standard method.
Ref 527982Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19.Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
Ref 529692Bioorg Med Chem. 2008 Oct 1;16(19):8781-94. Epub 2008 Aug 29.Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
Ref 528065Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.
Ref 530746J Med Chem. 2010 Mar 25;53(6):2622-35.Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.
Ref 529102Bioorg Med Chem. 2008 Jan 1;16(1):530-5. Epub 2007 Sep 14.Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.
Ref 530746J Med Chem. 2010 Mar 25;53(6):2622-35.Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.
Ref 530746J Med Chem. 2010 Mar 25;53(6):2622-35.Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.

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