Proteins > Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A
Page last updated: 2024-08-07 16:50:36
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A
A dual specificity calcium/calmodulin-dependent 3,5-cyclic nucleotide phosphodiesterase 1A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P54750]
Synonyms
Cam-PDE 1A;
EC 3.1.4.17;
61 kDa Cam-PDE;
hCam-1
Research
Bioassay Publications (30)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 7 (23.33) | 18.7374 |
| 1990's | 7 (23.33) | 18.2507 |
| 2000's | 8 (26.67) | 29.6817 |
| 2010's | 5 (16.67) | 24.3611 |
| 2020's | 3 (10.00) | 2.80 |
Compounds (35)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| rolipram | Homo sapiens (human) | IC25 | 1,400.0000 | 1 | 2 |
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
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 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
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. 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
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-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
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. 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
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
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
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
Identification of a potent new chemotype for the selective inhibition of PDE4.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
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
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
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. 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. 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
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
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
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Synthesis and biological evaluation of Vinpocetine derivatives.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
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
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
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, 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
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.Bioorganic & medicinal chemistry, , May-01, Volume: 23, Issue:9, 2015
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
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
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
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
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
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
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
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
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reactions: 3',5'-cyclic AMP + H2O = AMP + H+ and 3',5'-cyclic GMP + H2O = GMP + H+; this activity is activated by binding to calcium-bound calmodulin. [PMID:8557689, PMID:9419816] |
| calmodulin binding | molecular function | Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activity | molecular function | Catalysis of the reactions: nucleoside 3',5'-cyclic GMP + H2O = GMP + H+; this activity is activated by binding to calcium-bound calmodulin. [GOC:jid] |
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 |
|---|
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| regulation of smooth muscle cell apoptotic process | biological process | Any process that modulates the frequency, rate, or extent of smooth muscle cell apoptotic process. [GOC:BHF, GOC:mtg_apoptosis, GOC:rl] |
| cGMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators] |
| regulation of smooth muscle cell proliferation | biological process | Any process that modulates the frequency, rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc] |
| 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] |