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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