Target Validation Information
TTD ID T88975
Target Name Phosphodiesterase 3A (PDE3A)
Type of Target
Successful
Drug Potency against Target Cilostazol Drug Info IC50 = 200 nM [10]
Milrinone Drug Info IC50 = 450 nM [10]
1,3,9,9a-Tetrahydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 100 nM [4]
1,3-Dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 500 nM [4]
1,3-Dihydro-naphtho[2,3-d]imidazol-2-one Drug Info IC50 = 7000 nM [4]
1,5-Dihydro-imidazo[2,1-b]quinazolin-2-one Drug Info IC50 = 8800 nM [7]
5-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 90 nM [4]
6-(2-Imidazol-1-yl-vinyl)-1H-quinolin-2-one Drug Info IC50 = 4000 nM [2]
6-Imidazol-1-yl-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 16000 nM [2]
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 4400 nM [2]
7-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 50 nM [4]
7-Ethoxy-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 20 nM [4]
7-Fluoro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 300 nM [4]
7-Iodo-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one Drug Info IC50 = 520 nM [7]
7-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 50 nM [4]
8-Chloro-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 300 nM [4]
8-Methyl-1,3-dihydro-imidazo[4,5-b]quinolin-2-one Drug Info IC50 = 10 nM [4]
BMY-20844 Drug Info IC50 = 13 nM [3]
CI-930 Drug Info IC50 = 400 nM [6]
Cilostazol Drug Info IC50 = 190 nM [8]
Enoximone Drug Info IC50 = 3800 nM [9]
IMAZODAN Drug Info IC50 = 4700 nM [2]
isobutylmethylxanthine Drug Info IC50 = 6900 nM [8]
KURAIDIN Drug Info IC50 = 1250 nM [1]
KURARINOL Drug Info IC50 = 2950 nM [1]
Ro 20-1724 Drug Info IC50 = 9100 nM [8]
SOPHOFLAVESCENOL Drug Info IC50 = 410 nM [1]
TETRAHYDROBENXIMIDAZOLE Drug Info IC50 = 110 nM [6]
VESNARINONE Drug Info IC50 = 10700 nM [5]
References
REF 1 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 2 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. J Med Chem. 1992 Feb 21;35(4):620-8.
REF 3 Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility. J Med Chem. 1992 Jul 10;35(14):2688-96.
REF 4 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation. J Med Chem. 1991 Sep;34(9):2906-16.
REF 5 Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors. Bioorg Med Chem. 2010 Jan 15;18(2):855-62.
REF 6 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)-pyridazi... J Med Chem. 1989 Feb;32(2):342-50.
REF 7 Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoim... J Med Chem. 1988 Nov;31(11):2136-45.
REF 8 A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. J Med Chem. 1985 May;28(5):537-45.
REF 9 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... J Med Chem. 1987 Feb;30(2):303-18.
REF 10 Re-discovering PDE3 inhibitors--new opportunities for a long neglected target. Curr Top Med Chem. 2007;7(4):421-36.

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