| 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 | [1] | |
| PKF-241-466 | Drug Info | IC50 = 141 nM | [2] | ||
| SR-973 | Drug Info | Ki = 4 nM | [3] | ||
| PKF-242-484 | Drug Info | IC50 = 56 nM | [2] | ||
| DPC-333 | Drug Info | IC50 = 17~100 nM | [4] | ||
| TMI-05 | Drug Info | IC50 = 140 nM | [5] | ||
| IK-682 | Drug Info | Ki = 0.56 nM | [6] | ||
| CIPEMASTAT | Drug Info | Ki = 230 nM | [7] | ||
| N-hydroxy-2-(4-methoxyphenylsulfonamido)acetamide | Drug Info | IC50 = 1800 nM | [8] | ||
| N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl) | Drug Info | IC50 = 110 nM | [1] | ||
| 2-(4-bromophenylsulfonamido)-N-hydroxyacetamide | Drug Info | IC50 = 3900 nM | [8] | ||
| 2-(biphenyl-4-ylsulfonamido)-N-hydroxyacetamide | Drug Info | IC50 = 2400 nM | [8] | ||
| References | |||||
| REF 1 | 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 2 | Bioorg Med Chem. 2009 Jan 15;17(2):444-59. Epub 2008 Dec 3.Current perspective of TACE inhibitors: a review. | ||||
| REF 3 | 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 4 | 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 5 | Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19.Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. | ||||
| REF 6 | 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 7 | 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 8 | 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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