Target Validation Information
Target ID T07663
Target Name CGMP-specific 3',5'-cyclic phosphodiesterase
Target Type
Successful
Drug Potency against Target SOPHOFLAVESCENOL Drug Info Ki = 5 nM [526395]
Benzo[1,3]dioxol-5-ylmethyl-quinazolin-4-yl-amine Drug Info IC50 = 4200 nM [533856]
KURARINOL Drug Info IC50 = 6100 nM [526395]
UK-371800 Drug Info IC50 = 4.2 nM [529766]
KURAIDIN Drug Info IC50 = 640 nM [526395]
ROLIPRAM Drug Info IC50 = 720 nM [533856]
ZAPRINAST Drug Info IC50 = 1110 nM [525827]
3,7-Bis(2-hydroxyethyl)icaritin Drug Info IC50 = 74 nM [529676]
UK-371800 Drug Info IC50 = 1.1 nM [529766]
SOPHORAFLAVANONE B Drug Info IC50 = 16230 nM [529676]
8-prenylapigenin Drug Info IC50 = 1290 nM [529676]
ICARIIN Drug Info IC50 = 5900 nM [529676]
Icariside II Drug Info IC50 = 160 nM [529676]
LORNEIC ACID A Drug Info IC50 = 12600 nM [530477]
BRL-61063 Drug Info Ki = 7500 nM [533908]
SK&F-96321 Drug Info IC50 = 1000 nM [533908]
SCH-57726 Drug Info IC50 = 190 nM
Trequinsin Drug Info IC50 = 5000 nM [533047]
8-prenylquercetin Drug Info IC50 = 700 nM [529676]
Cartazolate Drug Info IC50 = 180 nM [526024]
ICARITIN Drug Info IC50 = 2200 nM [529676]
7-(2-Hydroxyethyl)-3-O-rhamnosylicariin Drug Info IC50 = 360 nM [529676]
References
Ref 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 533856J Med Chem. 1994 Jun 24;37(13):2106-11.Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
Ref 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 529766Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6. Epub 2008 Oct 11.Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
Ref 526395Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Ref 533856J Med Chem. 1994 Jun 24;37(13):2106-11.Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
Ref 525827J Med Chem. 2000 Jun 29;43(13):2523-9.4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 529766Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6. Epub 2008 Oct 11.Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 530477J Nat Prod. 2009 Nov;72(11):2046-8.Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete.
Ref 533908J Med Chem. 1994 Feb 18;37(4):476-85.Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Ref 533908J Med Chem. 1994 Feb 18;37(4):476-85.Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Ref 533047J Med Chem. 1989 Jul;32(7):1450-7.Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 526024J Med Chem. 2001 Mar 29;44(7):1025-7.Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Ref 529676J Nat Prod. 2008 Sep;71(9):1513-7. Epub 2008 Sep 9.Potent inhibition of human phosphodiesterase-5 by icariin derivatives.

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