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 529102 | Bioorg 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 529876 | Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review. | ||||
Ref 528025 | Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. | ||||
Ref 529876 | Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review. | ||||
Ref 534251 | J 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 527982 | Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19.Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. | ||||
Ref 529692 | Bioorg 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 528065 | Bioorg 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 530746 | J 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 529102 | Bioorg 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 530746 | J 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 530746 | J 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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