Target Validation Information
TTD ID	T07663
Target Name	Phosphodiesterase 5A (PDE5A)
Type of Target	Successful
Drug Potency against Target		Drug Info	IC50 = 1000 nM	[9]
	3,7-Bis(2-hydroxyethyl)icaritin	Drug Info	IC50 = 74 nM	[4]
	7-(2-Hydroxyethyl)-3-O-rhamnosylicariin	Drug Info	IC50 = 360 nM	[4]
	8-prenylapigenin	Drug Info	IC50 = 1290 nM	[4]
	8-prenylquercetin	Drug Info	IC50 = 700 nM	[4]
	Benzo[1,3]dioxol-5-ylmethyl-quinazolin-4-yl-amine	Drug Info	IC50 = 4200 nM	[8]
	BRL-61063	Drug Info	Ki = 7500 nM	[9]
	Cartazolate	Drug Info	IC50 = 180 nM	[2]
	ICARIIN	Drug Info	IC50 = 5900 nM	[4]
	Icariside II	Drug Info	IC50 = 160 nM	[4]
	ICARITIN	Drug Info	IC50 = 2200 nM	[4]
	KURAIDIN	Drug Info	IC50 = 640 nM	[3]
	KURARINOL	Drug Info	IC50 = 6100 nM	[3]
	LORNEIC ACID A	Drug Info	IC50 = 12600 nM	[6]
	ROLIPRAM	Drug Info	IC50 = 720 nM	[8]
	SCH-57726	Drug Info	IC50 = 190 nM
	SOPHOFLAVESCENOL	Drug Info	Ki = 5 nM	[3]
	SOPHORAFLAVANONE B	Drug Info	IC50 = 16230 nM	[4]
	Trequinsin	Drug Info	IC50 = 5000 nM	[7]
	UK-371800	Drug Info	IC50 = 4.2 nM	[5]
	UK-371800	Drug Info	IC50 = 1.1 nM	[5]
	ZAPRINAST	Drug Info	IC50 = 1110 nM	[1]
References
REF 1	4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. J Med Chem. 2000 Jun 29;43(13):2523-9.
REF 2	Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. J Med Chem. 2001 Mar 29;44(7):1025-7.
REF 3	A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.
REF 4	Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
REF 5	Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6.
REF 6	Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete. J Nat Prod. 2009 Nov;72(11):2046-8.
REF 7	Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues. J Med Chem. 1989 Jul;32(7):1450-7.
REF 8	Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. J Med Chem. 1994 Jun 24;37(13):2106-11.
REF 9	Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.

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