Target Validation Information
TTD ID T20178
Target Name Tumor necrosis factor (TNF)
Type of Target
Successful
Drug Potency against Target Infliximab Drug Info IC50 = 37ng = ml [5]
Lenalidomide Drug Info IC50 = 5000 nM [4]
Pentoxifylline Drug Info IC50 = 100000 nM [7]
Pirenzepine Drug Info IC50 = 30.7 ug/ml [3]
Thalidomide Drug Info IC50 = 194000 nM
AN0128 Drug Info Ki = 40.0 nM [6]
Pirfenidone Drug Info IC50 = 30.7 ug/ml [3]
IK-862 Drug Info IC50 = 0.35 nM [2]
PKF-241-466 Drug Info IC50 = 269 nM [1]
PKF-242-484 Drug Info IC50 = 48 nM [1]
References
REF 1 Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. J Med Chem. 2002 May 23;45(11):2289-93.
REF 2 Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structu... J Med Chem. 2002 Nov 7;45(23):4954-7.
REF 3 Inhibition of experimental acute pulmonary inflammation by pirfenidone. Pulm Pharmacol Ther. 2003;16(4):207-14.
REF 4 Targeting 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.
REF 5 Dominant-negative inhibitors of soluble TNF attenuate experimental arthritis without suppressing innate immunity to infection. J Immunol. 2007 Aug 1;179(3):1872-83.
REF 6 Dopamine D5 receptors: a challenge to medicinal chemists. Mini Rev Med Chem. 2008 Sep;8(10):976-95.
REF 7 Beneficial 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.

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