Target Validation Information
Target ID T88975
Target Name CGMP-inhibited 3',5'-cyclic phosphodiesterase A
Target Type
Successful
Drug Potency against Target Milrinone Drug Info IC50 = 450 nM [552676]
Ro 20-1724 Drug Info IC50 = 9100 nM [533395]
8-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 10 nM [528087]
7-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 50 nM [528087]
IMAZODAN Drug Info IC50 = 4700 nM [526726]
8-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 300 nM [528087]
OPC-13013 Drug Info IC50 = 190 nM [533395]
1,3-Dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 500 nM [528087]
7-Fluoro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 300 nM [528087]
7-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 50 nM [528087]
1,3-Dihydro-naphtho[2,3-d]imidazol-2-one Drug Info IC50 = 7000 nM [528087]
VESNARINONE Drug Info IC50 = 10700 nM [530575]
TETRAHYDROBENXIMIDAZOLE Drug Info IC50 = 110 nM [533015]
6-(2-Imidazol-1-yl-vinyl)-1H-quinolin-2-one Drug Info IC50 = 4000 nM [526726]
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 4400 nM [526726]
Cilostazol Drug Info IC50 = 200 nM [552676]
SOPHOFLAVESCENOL Drug Info IC50 = 410 nM [526395]
6-Imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 16000 nM [526726]
1,5-Dihydro-imidazo[2,1-b]quinazolin-2-one Drug Info IC50 = 8800 nM [533367]
7-Ethoxy-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 20 nM [528087]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info IC50 = 6900 nM [533395]
7-Iodo-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one Drug Info IC50 = 520 nM [533367]
BMY-20844 Drug Info IC50 = 13 nM [526741]
1,3,9,9a-Tetrahydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 100 nM [528087]
CI-930 Drug Info IC50 = 400 nM [533015]
KURARINOL Drug Info IC50 = 2950 nM [526395]
KURAIDIN Drug Info IC50 = 1250 nM [526395]
FENOXIMONE Drug Info IC50 = 3800 nM [533411]
5-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 90 nM [528087]
References
Ref 552676Re-discovering PDE3 inhibitors--new opportunities for a long neglected target. Curr Top Med Chem. 2007;7(4):421-36.
Ref 533395J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 526726J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 533395J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 530575Bioorg Med Chem. 2010 Jan 15;18(2):855-62. Epub 2009 Nov 26.Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors.
Ref 533015J Med Chem. 1989 Feb;32(2):342-50.Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure.
Ref 526726J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Ref 526726J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Ref 552676Re-discovering PDE3 inhibitors--new opportunities for a long neglected target. Curr Top Med Chem. 2007;7(4):421-36.
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 526726J Med Chem. 1992 Feb 21;35(4):620-8.3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Ref 533367J Med Chem. 1988 Nov;31(11):2136-45.Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 533395J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
Ref 533367J Med Chem. 1988 Nov;31(11):2136-45.Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
Ref 526741J Med Chem. 1992 Jul 10;35(14):2688-96.Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility.
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.
Ref 533015J Med Chem. 1989 Feb;32(2):342-50.Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure.
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 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 533411J Med Chem. 1987 Feb;30(2):303-18.Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856).
Ref 528087J Med Chem. 1991 Sep;34(9):2906-16.1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.

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