Target Validation Information
TTD ID	T67619
Target Name	RAC-alpha serine/threonine-protein kinase (AKT1)
Type of Target	Successful
Drug Potency against Target	CI-1033	Drug Info	IC50 = 19 nM
	Enzastaurin	Drug Info	IC50 = 30 nM	[7]
	MK-2206	Drug Info	IC50 = 8~65 nM	[8]
	RX-0201	Drug Info	IC50 = 100 nM
	XL418	Drug Info	IC50 = 20 nM
	(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one	Drug Info	IC50 = 3000 nM	[3]
	4,5,6-trihydroxy-3-methylphthalide	Drug Info	IC50 = 19700 nM	[1]
	A-443654	Drug Info	IC50 = 0.16 nM	[2]
	BMS-754807	Drug Info	IC50 = 22 nM	[5]
	BX-517	Drug Info	IC50 = 100 nM	[3]
	SB-747651A	Drug Info	IC50 = 200 nM	[4]
Action against Disease Model	Perifosine	Drug Info	Perifosine showed single agent anti-proliferative activity in a variety of gastric cancer cell lines. In 8/13 cell lines resistant to 5-FU, perifosine showed a synergistic antiproliferative activity with 5-FU. In 72% of cell lines, high basal levels of pAkt were detected. Treatment with perifosine reduced t uMor growth in nude mice inoculated subcutaneously with the YCC 2 gastric cancer cell line. The Akt inhibitor Perifosine strongly enhances the antit uMor and antivascular activity of CD34+ cells engineered to express membrane-bound TRAIL	[6]
References
REF 1	A phthalide with in vitro growth inhibitory activity from an oidiodendron strain. J Nat Prod. 2004 Dec;67(12):2086-9.
REF 2	Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem. 2007 Jun 28;50(13):2990-3003.
REF 3	Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.
REF 4	Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-o... J Med Chem. 2008 Sep 25;51(18):5663-79.
REF 5	Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in cli... J Med Chem. 2009 Dec 10;52(23):7360-3.
REF 6	Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.
REF 7	Small molecule inhibitors of PKCTheta as potential antiinflammatory therapeutics. Curr Top Med Chem. 2009;9(7):640-54.
REF 8	The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation: a 2009 update. Curr Top Med Chem. 2010;10(4):458-77.

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