Proteins > cGMP-specific 3',5'-cyclic phosphodiesterase
Page last updated: 2024-08-07 15:28:08
cGMP-specific 3',5'-cyclic phosphodiesterase
A cGMP-specific 3,5-cyclic phosphodiesterase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O76074]
Synonyms
EC 3.1.4.35;
cGMP-binding cGMP-specific phosphodiesterase;
CGB-PDE
Research
Bioassay Publications (83)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (3.61) | 18.7374 |
| 1990's | 9 (10.84) | 18.2507 |
| 2000's | 35 (42.17) | 29.6817 |
| 2010's | 27 (32.53) | 24.3611 |
| 2020's | 9 (10.84) | 2.80 |
Compounds (57)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tadalafil | Homo sapiens (human) | EC50 | 5.8100 | 1 | 1 |
| sildenafil | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| rolipram | Homo sapiens (human) | IC25 | 1,400.0000 | 1 | 1 |
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
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
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
[no title available],
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
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development.The Journal of biological chemistry, , Jul-28, Volume: 281, Issue:30, 2006
Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents.Journal of medicinal chemistry, , Oct-25, Volume: 44, Issue:22, 2001
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
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 GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 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
Aryl sulfonamides as selective PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
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
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Multi-target design strategies for the improved treatment of Alzheimer's disease.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
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
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
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
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
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
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.European journal of medicinal chemistry, , Volume: 45, Issue:4, 2010
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
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
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
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 13, Issue:8, 2003
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
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
Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
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
Computational design, synthesis and biological evaluation of PDE5 inhibitors based on NBioorganic & medicinal chemistry, , 12-15, Volume: 76, 2022
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.RSC medicinal chemistry, , Nov-16, Volume: 13, Issue:11, 2022
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
[no title available]Journal of medicinal chemistry, , 09-10, Volume: 63, Issue:17, 2020
Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model.European journal of medicinal chemistry, , Sep-01, Volume: 177, 2019
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
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
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
[no title available]European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
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
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
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
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.The Journal of biological chemistry, , Apr-06, Volume: 287, Issue:15, 2012
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.Journal of natural products, , Volume: 71, Issue:9, 2008
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction.Journal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development.The Journal of biological chemistry, , Jul-28, Volume: 281, Issue:30, 2006
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
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
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.Bioorganic & medicinal chemistry letters, , Jun-02, Volume: 15, Issue:11, 2005
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 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
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
Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
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
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Mar-29, Volume: 44, Issue:7, 2001
The discovery of novel, potent and selective PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
[no title available],
New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
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
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 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
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.Journal of medicinal chemistry, , Nov-26, Volume: 36, Issue:24, 1993
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
[no title available],
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.Journal of medicinal chemistry, , 08-09, Volume: 61, Issue:15, 2018
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.Journal of medicinal chemistry, , 02-08, Volume: 61, Issue:3, 2018
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
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
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
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
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
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
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.Bioorganic & medicinal chemistry, , Aug-15, Volume: 16, Issue:16, 2008
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
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
Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Enables
This protein enables 6 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] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| cGMP binding | molecular function | Binding to cGMP, the nucleotide cyclic GMP (guanosine 3',5'-cyclophosphate). [GOC:ai] |
| 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] |
| 3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| 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] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cellular_component | cellular component | A location, relative to cellular compartments and structures, occupied by a macromolecular machine. There are three types of cellular components described in the gene ontology: (1) the cellular anatomical entity where a gene product carries out a molecular function (e.g., plasma membrane, cytoskeleton) or membrane-enclosed compartments (e.g., mitochondrion); (2) virion components, where viral proteins act, and (3) the stable macromolecular complexes of which gene product are parts (e.g., the clathrin complex). [GOC:pdt] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| positive regulation of cardiac muscle hypertrophy | biological process | Any process that increases the rate, frequency or extent of the enlargement or overgrowth of all or part of the heart due to an increase in size (not length) of individual cardiac muscle fibers, without cell division. [GOC:BHF, GOC:dph, GOC:tb] |
| regulation of nitric oxide mediated signal transduction | biological process | Any process that modulates the rate, frequency or extent of nitric oxide mediated signal transduction. Nitric oxide mediated signal transduction is The series of molecular signals mediated by the detection of nitric oxide (NO). [GOC:BHF, GOC:dph, GOC:tb] |
| T cell proliferation | biological process | The expansion of a T cell population by cell division. Follows T cell activation. [GOC:jl] |
| negative regulation of T cell proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of T cell proliferation. [GOC:jl] |
| cGMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators] |
| oocyte development | biological process | The process whose specific outcome is the progression of an oocyte over time, from initial commitment of the cell to its specific fate, to the fully functional differentiated cell. [GOC:go_curators] |
| negative regulation of cardiac muscle contraction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cardiac muscle contraction. [GOC:ecd] |
| relaxation of cardiac muscle | biological process | The process in which the extent of cardiac muscle contraction is reduced. [GOC:ecd] |
| positive regulation of oocyte development | biological process | Any process that increases the rate or extent of the process whose specific outcome is the progression of an oocyte over time, from initial commitment of the cell to its specific fate, to the fully functional differentiated cell. [GOC:dph, GOC:tb] |
| 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] |