Proteins > cGMP-inhibited 3',5'-cyclic phosphodiesterase B
Page last updated: 2024-08-07 17:05:28
cGMP-inhibited 3',5'-cyclic phosphodiesterase B
A cGMP-inhibited 3,5-cyclic phosphodiesterase 3B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13370]
Synonyms
EC 3.1.4.17;
CGIPDE1;
CGIP1;
Cyclic GMP-inhibited phosphodiesterase B;
CGI-PDE B
Research
Bioassay Publications (79)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 18 (22.78) | 18.7374 |
1990's | 19 (24.05) | 18.2507 |
2000's | 27 (34.18) | 29.6817 |
2010's | 14 (17.72) | 24.3611 |
2020's | 1 (1.27) | 2.80 |
Compounds (58)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
my 5445 | Homo sapiens (human) | Ki | 16.0000 | 1 | 1 |
theophylline | Homo sapiens (human) | IC50 | 300.0000 | 2 | 2 |
cilostamide | Homo sapiens (human) | IC50 | 0.0502 | 5 | 6 |
cilostamide | Homo sapiens (human) | Ki | 0.0125 | 2 | 2 |
cilostazol | Homo sapiens (human) | IC50 | 0.4367 | 3 | 3 |
dipyridamole | Homo sapiens (human) | IC50 | 43.0000 | 1 | 1 |
etazolate | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
amrinone | Homo sapiens (human) | IC50 | 52.8750 | 8 | 8 |
1-methyl-3-isobutylxanthine | Homo sapiens (human) | IC50 | 0.2420 | 2 | 2 |
losartan | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
milrinone | Homo sapiens (human) | IC50 | 2.2896 | 23 | 24 |
milrinone | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
papaverine | Homo sapiens (human) | IC50 | 1.0300 | 1 | 1 |
papaverine | Homo sapiens (human) | Ki | 0.2825 | 2 | 4 |
proxyphylline | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone | Homo sapiens (human) | IC50 | 300.0000 | 1 | 1 |
rolipram | Homo sapiens (human) | IC50 | 145.1835 | 11 | 20 |
rolipram | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
sulmazole | Homo sapiens (human) | IC50 | 383.3333 | 3 | 3 |
vesnarinone | Homo sapiens (human) | IC50 | 11.3133 | 3 | 3 |
zardaverine | Homo sapiens (human) | IC50 | 71.4120 | 5 | 14 |
9-benzyladenine | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
eg 626 | Homo sapiens (human) | Ki | 1.4000 | 1 | 1 |
enoximone | Homo sapiens (human) | IC50 | 11.4500 | 4 | 4 |
piroximone | Homo sapiens (human) | IC50 | 39.0667 | 3 | 3 |
2-(2-methoxy-4-(methylsulfinyl)phenyl)-1h-imidazo(4,5-c)pyridine | Homo sapiens (human) | IC50 | 42.0000 | 1 | 1 |
imazodan | Homo sapiens (human) | IC50 | 16.1182 | 11 | 11 |
nitraquazone | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
tadalafil | Homo sapiens (human) | IC50 | 65.9536 | 7 | 17 |
y 590 | Homo sapiens (human) | IC50 | 0.1100 | 2 | 2 |
9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
cilomilast | Homo sapiens (human) | IC50 | 41.1570 | 4 | 14 |
rp 73401 | Homo sapiens (human) | IC50 | 36.7900 | 1 | 10 |
8-methoxymethyl-3-isobutyl-1-methylxanthine | Homo sapiens (human) | IC50 | 240.0000 | 1 | 1 |
vinpocetine | Homo sapiens (human) | IC50 | 300.0000 | 1 | 1 |
rolipram | Homo sapiens (human) | IC50 | 3.1623 | 1 | 1 |
roflumilast | Homo sapiens (human) | IC50 | 124.2002 | 1 | 10 |
4,5-dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2h)-pyridazinone | Homo sapiens (human) | IC50 | 0.5500 | 8 | 8 |
indolidan | Homo sapiens (human) | IC50 | 3.5400 | 2 | 2 |
bemoradan | Homo sapiens (human) | IC50 | 0.3000 | 2 | 2 |
1,3-dihydro-7,8-dimethyl-2h-imidazo(4,5-b)quinolin-2-one | Homo sapiens (human) | IC50 | 0.0110 | 3 | 3 |
ci 1044 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
t 1032 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
losartan potassium | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
pf 04217903 | Homo sapiens (human) | IC50 | 3.3300 | 2 | 2 |
3-(2,5-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine | Homo sapiens (human) | IC50 | 0.7200 | 1 | 1 |
pf-04418948 | Homo sapiens (human) | IC50 | 3.5000 | 1 | 0 |
nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
an2728 | Homo sapiens (human) | IC50 | 29,403.2000 | 2 | 2 |
cc-115 | Homo sapiens (human) | IC50 | 0.6300 | 1 | 1 |
chf6001 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
cyclic gmp | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
sildenafil | Homo sapiens (human) | IC50 | 28.7106 | 10 | 19 |
zaprinast | Homo sapiens (human) | IC50 | 391.0000 | 2 | 2 |
vardenafil | Homo sapiens (human) | IC50 | 6.1984 | 3 | 12 |
Imidazosagatriazinone | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
bl 4162a | Homo sapiens (human) | IC50 | 0.2327 | 6 | 6 |
1,5-dihydro-7-(1-piperidinyl)-imidazo(2,1-b)quinazolin-2(3h)-one | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
quazinone | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
lixazinone | Homo sapiens (human) | IC50 | 0.0083 | 4 | 4 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
rolipram | Homo sapiens (human) | Log IC50 | 0.0040 | 1 | 1 |
Discovery of new inhibitor for PDE3 by virtual screening.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Synthesis and in vitro antiplatelet activity of new 4-(1-piperazinyl)coumarin derivatives. Human platelet phosphodiesterase 3 inhibitory properties of the two most effective compounds described and molecular modeling study on their interactions with phospJournal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
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 tJournal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Synthesis and cardiotonic activity of a series of substituted 4-alkyl-2(1H)-quinazolinones.Journal of medicinal chemistry, , Volume: 30, Issue:8, 1987
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlJournal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Bipyridine cardiotonics: the three-dimensional structures of amrinone and milrinone.Journal of medicinal chemistry, , Volume: 29, Issue:5, 1986
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity.Biochemistry, , May-25, Volume: 43, Issue:20, 2004
Synthesis and evaluation of novel 2-pyridone derivatives as inhibitors of phosphodiesterase3 (PDE3): a target for heart failure and platelet aggregation.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 22, Issue:18, 2012
Synthesis and in vitro antiplatelet activity of new 4-(1-piperazinyl)coumarin derivatives. Human platelet phosphodiesterase 3 inhibitory properties of the two most effective compounds described and molecular modeling study on their interactions with phospJournal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
Studies of cardiotonic agents. 8. Synthesis and biological activities of optically active 6-(4-(benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl-3(2H)- pyridazinone (KF15232).Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Novel cAMP PDE III inhibitors: 1,6-naphthyridin-2(1H)-ones.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
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 tJournal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3 (2H)-isoquinolinones and related compounds. Synthesis and activity.Journal of medicinal chemistry, , Volume: 32, Issue:2, 1989
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.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlJournal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 5. 1,2-Dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-6-methyl-2-oxo-3- pyridinecarbonitriles and related compounds. Synthesis and inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:6, 1987
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).Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Bipyridine cardiotonics: the three-dimensional structures of amrinone and milrinone.Journal of medicinal chemistry, , Volume: 29, Issue:5, 1986
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
New analgesic drugs derived from phencyclidine.Journal of medicinal chemistry, , Volume: 24, Issue:5, 1981
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Synthesis and biological evaluation of 2,5-dihydropyrazol.Bioorganic & medicinal chemistry letters, , Dec-04, Volume: 10, Issue:23, 2000
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
Design and discovery of 2-(4-(1H-tetrazol-5-yl)-1H-pyrazol-1-yl)-4-(4-phenyl)thiazole derivatives as cardiotonic agents via inhibition of PDE3.Bioorganic & medicinal chemistry, , Sep-15, Volume: 23, Issue:18, 2015
Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
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).Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
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).Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
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.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.Journal of medicinal chemistry, , Feb-21, Volume: 35, Issue:4, 1992
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
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 tJournal of medicinal chemistry, , Volume: 32, Issue:2, 1989
Chemistry and positive inotropic effect of pelrinone and related derivatives. A novel class of 2-methylpyrimidones as inotropic agents.Journal of medicinal chemistry, , Volume: 31, Issue:4, 1988
Cardiotonic agents. 6. Synthesis and inotropic activity of 2,4-dihydro-5-[4-(1H-imidazol-1-yl)phenyl]-3H-pyrazol-3-ones: ring-contracted analogues of imazodan (CI-914).Journal of medicinal chemistry, , Volume: 30, Issue:10, 1987
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlJournal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 3. Synthesis and biological activity of novel 6-(substituted 1H-imidazol-4(5)-yl)-3(2H)-pyridazinones.Journal of medicinal chemistry, , Volume: 29, Issue:2, 1986
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
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 tJournal of medicinal chemistry, , Volume: 32, Issue:2, 1989
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.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
Cardiotonic agents. 7. Inhibition of separated forms of cyclic nucleotide phosphodiesterase from guinea pig cardiac muscle by 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones and related compounds. Structure-activity relationships and correlJournal of medicinal chemistry, , Volume: 30, Issue:11, 1987
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).Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Cardiotonic agents. 4. Synthesis and biological evaluation of N-substituted 2,4,4a,5-tetrahydro-3H-indeno[1,2-c]pyridazin-3-ones: rigid structures derived from CI-930 and analogues.Journal of medicinal chemistry, , Volume: 29, Issue:11, 1986
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.Journal of medicinal chemistry, , Volume: 27, Issue:9, 1984
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Heteroatom analogues of bemoradan: chemistry and cardiotonic activity of 1,4-benzothiazinylpyridazinones.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 15, Issue:7, 2005
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-25, Volume: 12, Issue:6, 2002
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.Journal of medicinal chemistry, , Jul-04, Volume: 40, Issue:14, 1997
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.Journal of medicinal chemistry, , Feb-21, Volume: 35, Issue:4, 1992
1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-ones--inhibitors of blood platelet cAMP phosphodiesterase and induced aggregation.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
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.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
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.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
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).Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Enables
This protein enables 7 target(s):
Target | Category | Definition |
3',5'-cyclic-nucleotide phosphodiesterase activity | molecular function | Catalysis of the reaction: a nucleoside 3',5'-cyclic phosphate + H2O = a nucleoside 5'-phosphate. [RHEA:14653] |
3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
cGMP-inhibited cyclic-nucleotide phosphodiesterase activity | molecular function | Catalysis of the reaction: nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate; catalytic activity is decreased in the presence of cGMP. [GOC:mah] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
protein kinase B binding | molecular function | Binding to protein kinase B, an intracellular kinase that is important in regulating glucose metabolism. [GOC:jl, http://www.heartandmetabolism.org/] |
metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
3',5'-cyclic-GMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic GMP + H2O = GMP + H+. [RHEA:16957] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
guanyl-nucleotide exchange factor complex | cellular component | A protein complex that stimulates the exchange of guanyl nucleotides associated with a GTPase. [GOC:mah] |
Involved In
This protein is involved in 9 target(s):
Target | Category | Definition |
angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
negative regulation of cell adhesion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell adhesion. [GOC:go_curators] |
G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
negative regulation of angiogenesis | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of angiogenesis. [GOC:go_curators] |
cellular response to insulin stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
negative regulation of cell adhesion mediated by integrin | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of cell adhesion mediated by integrin. [GOC:add] |
negative regulation of lipid catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of an adenylate cyclase-activating G protein-coupled receptor signaling pathway. [GOC:hjd, PMID:19246489] |
cAMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic AMP (cAMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |