| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T20178 | ||||
| Target Name | Tumor necrosis factor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Pentoxifylline | Drug Info | IC50 = 100000 nM | [553186] | |
| Infliximab | Drug Info | IC50 = 37ng = ml | [552721] | ||
| PKF-241-466 | Drug Info | IC50 = 269 nM | [526335] | ||
| PKF-242-484 | Drug Info | IC50 = 48 nM | [526335] | ||
| Lenalidomide | Drug Info | IC50 = 5000 nM | [552648] | ||
| AN0128 | Drug Info | Ki = 40.0 nM | [552866] | ||
| Pirenzepine | Drug Info | IC50 = 30.7 ug/ml | [552355] | ||
| IK-682 | Drug Info | IC50 = 0.35 nM | [526446] | ||
| Pirfenidone | Drug Info | IC50 = 30.7 ug/ml | [552355] | ||
| Thalidomide | Drug Info | IC50 = 194000 nM | |||
| References | |||||
| Ref 553186 | 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. | ||||
| Ref 552721 | 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 526335 | J 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 526335 | J 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 552648 | 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. Epub 2006 Oct 5. | ||||
| Ref 552866 | Dopamine D5 receptors: a challenge to medicinal chemists. Mini Rev Med Chem. 2008 Sep;8(10):976-95. | ||||
| Ref 552355 | Inhibition of experimental acute pulmonary inflammation by pirfenidone. Pulm Pharmacol Ther. 2003;16(4):207-14. | ||||
| Ref 526446 | J 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. | ||||
| Ref 552355 | Inhibition of experimental acute pulmonary inflammation by pirfenidone. Pulm Pharmacol Ther. 2003;16(4):207-14. | ||||
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