Target Validation Information
Target ID T20178
Target Name Tumor necrosis factor
Target Type
Successful
Drug Potency against Target Pentoxifylline Drug Info IC50 = 100000 nM [1]
Infliximab Drug Info IC50 = 37ng = ml [2]
PKF-241-466 Drug Info IC50 = 269 nM [3]
PKF-242-484 Drug Info IC50 = 48 nM [3]
Lenalidomide Drug Info IC50 = 5000 nM [4]
AN0128 Drug Info Ki = 40.0 nM [5]
Pirenzepine Drug Info IC50 = 30.7 ug/ml [6]
IK-682 Drug Info IC50 = 0.35 nM [7]
Pirfenidone Drug Info IC50 = 30.7 ug/ml [6]
Thalidomide Drug Info IC50 = 194000 nM
References
REF 1Beneficial effects of the phosphodiesterase inhibitors BRL 61063, pentoxifylline, and rolipram in a murine model of endotoxin shock. Circ Shock. 1994 Dec;44(4):188-95.
REF 2Dominant-negative inhibitors of soluble TNF attenuate experimental arthritis without suppressing innate immunity to infection. J Immunol. 2007 Aug 1;179(3):1872-83.
REF 3J Med Chem. 2002 May 23;45(11):2289-93.Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme.
REF 4Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood. 2007 Feb 15;109(4):1669-77. Epub 2006 Oct 5.
REF 5Dopamine D5 receptors: a challenge to medicinal chemists. Mini Rev Med Chem. 2008 Sep;8(10):976-95.
REF 6Inhibition of experimental acute pulmonary inflammation by pirfenidone. Pulm Pharmacol Ther. 2003;16(4):207-14.
REF 7J Med Chem. 2002 Nov 7;45(23):4954-7.Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.

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