Target Validation Information
TTD ID	T23172
Target Name	Janus kinase 3 (JAK-3)
Type of Target	Successful
Drug Potency against Target	Tofacitinib	Drug Info	IC50 = 1 nM	[4]
	6-o-tolylquinazolin-2-amine	Drug Info	IC50 = 9819 nM	[1]
	Atropisomer 1	Drug Info	IC50 = 1530 nM	[2]
Action against Disease Model	Tofacitinib	Drug Info	A specific orally active inhibitor of JAK3, CP-690,550, significantly prolonged survival in a murine model of heart transplantation and in cynomolgus monkeys receiving kidney transplants. CP-690,550 treatment was not associated with hypertension, hyperlipidemia, or lymphoproliferative disease. On the basis of these preclinical results, we believe JAK3 blockade by CP-690,550 has potential for therapeutically desirable immunosuppression in h uMan organ transplantation and in other clinical setting	[3]
References
REF 1	Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. J Med Chem. 2006 Sep 21;49(19):5671-86.
REF 2	Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. J Med Chem. 2009 Dec 24;52(24):7938-41.
REF 3	Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003 Oct 31;302(5646):875-8.
REF 4	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.

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