Target Validation Information
TTD ID	T93515
Target Name	P2Y purinoceptor 2 (P2RY2)
Type of Target	Clinical trial
Drug Potency against Target	Diquafosol	Drug Info	EC50 = 100 nM	[4]
	Acid blue 25	Drug Info	IC50 = 11000 nM	[2]
	PSB-0963	Drug Info	IC50 = 10000 nM	[2]
	PSB-716	Drug Info	IC50 = 9000 nM	[1]
	RB 2	Drug Info	IC50 = 5000 nM	[1]
	SB-416	Drug Info	IC50 = 17000 nM	[1]
Action against Disease Model	Diquafosol	Drug Info	In primate lung tissues, the P2Y(2) receptor mRNA was located by in situ hybridization predominantly in epithelial cells and not in smooth muscle or stromal tissue. The pharmacologic profile of INS37217 parallels that of UTP, leading to increased chloride and water secretion, increased cilia beat frequency, and increased mucin release.	[3]
References
REF 1	Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7.
REF 2	Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold. J Med Chem. 2010 Mar 11;53(5):2076-86.
REF 3	Pharmacology of INS37217 [P(1)-(uridine 5')-P(4)- (2'-deoxycytidine 5')tetraphosphate, tetrasodium salt], a next-generation P2Y(2) receptor agonist for the treatment of cystic fibrosis. J Pharmacol Exp Ther. 2002 Sep;302(3):871-80.
REF 4	Novel nucleotide triphosphates as potent P2Y2 agonists. Bioorg Med Chem Lett. 2007 Jan 15;17(2):562-5.

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