Target Validation Information
TTD ID	T94479
Target Name	Ribosomal protein S6 kinase beta-1 (S6K1)
Type of Target	Clinical trial
Drug Potency against Target	4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	Drug Info	IC50 = 10000 nM	[3]
	PHA-767491	Drug Info	IC50 = 3010 nM	[4]
	Ro31-8220	Drug Info	IC50 = 8 nM	[1]
	SB-747651A	Drug Info	IC50 = 0.5 nM	[2]
Action against Disease Model	XL418	Drug Info	XL418 potently inhibits the activity of AKT and S6K in preclinical models, reducing t uMor growth and enhancing the effects of other targeted therapies. XL418 slowed t uMor growth in multiple cancer models, including breast and lung adenocarcinomas. XL418 also has been shown to enhance apoptosis in combination with XL647, an inhibitor of multiple receptor tyrosine kinases including EGFR, HER2, and VEGFR, in preclinical t uMor models.
References
REF 1	Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
REF 2	(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3407-11.
REF 3	4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
REF 4	Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.

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