Target Validation Information
TTD ID	T81443
Target Name	Toll-like receptor 4 (TLR4)
Type of Target	Clinical trial
Drug Potency against Target	Resatorvid	Drug Info	IC50 = 5.5 nM	[3]
	6-(2-aminophenoxy)benzo[d]isothiazol-3-amine	Drug Info	IC50 = 3000 nM	[1]
	CRX-526	Drug Info	IC50 = 2.4 nM	[2]
	ERITORAN	Drug Info	IC50 = 1.5 nM	[1]
Action against Disease Model	Resatorvid	Drug Info	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	[3]
References
REF 1	Small molecule modulators of toll-like receptors. J Med Chem. 2008 Nov 13;51(21):6621-6.
REF 2	The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5350-4.
REF 3	TAK-242 selectively suppresses Toll-like receptor 4-signaling mediated by the intracellular domain. Eur J Pharmacol. 2008 Apr 14;584(1):40-8.

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