| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T81443 | ||||
| Target Name | Toll-like receptor 4 | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | CRX-526 | Drug Info | IC50 = 2.4 nM | [529737] | |
| ERITORAN | Drug Info | IC50 = 1.5 nM | [529731] | ||
| 6-(2-aminophenoxy)benzo[d]isothiazol-3-amine | Drug Info | IC50 = 3000 nM | [529731] | ||
| Resatorvid | Drug Info | IC50 = 5.5 nM | [536637] | ||
| Action against Disease Model | Resatorvid | TAK-242 (resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4. TAK-242 almost completely suppressed production of nitric oxide (NO) or t uMor necrosis factor (TNF)-alpha induced by a TLR4-specific ligand, ultra-pure LPS, in mouse RAW264.7, h uMan U-937 and P31/FUJ cells. AK-242 potently inhibited nuclear factor (NF)-kappaB activation induced by ultra-pure LPS in HEK293 cells transiently expressing TLR4 and co-receptors, myeloid differentiation protein-2 (MD2) and CD14. TAK-242 potently inhibited the signaling from CD4-TLR4 chimera receptors | [536637] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Gene deletion resulted in Eosinophilia and Immune response decrease compared with wild type | [529737] | |||
| References | |||||
| Ref 529737 | Bioorg Med Chem Lett. 2008 Oct 15;18(20):5350-4. Epub 2008 Sep 19.The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics. | ||||
| Ref 529731 | J Med Chem. 2008 Nov 13;51(21):6621-6. Epub 2008 Oct 2.Small molecule modulators of toll-like receptors. | ||||
| Ref 536637 | TAK-242 selectively suppresses Toll-like receptor 4-signaling mediated by the intracellular domain. Eur J Pharmacol. 2008 Apr 14;584(1):40-8. Epub 2008 Feb 5. | ||||
| Ref 529731 | J Med Chem. 2008 Nov 13;51(21):6621-6. Epub 2008 Oct 2.Small molecule modulators of toll-like receptors. | ||||
| Ref 536637 | TAK-242 selectively suppresses Toll-like receptor 4-signaling mediated by the intracellular domain. Eur J Pharmacol. 2008 Apr 14;584(1):40-8. Epub 2008 Feb 5. | ||||
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