Proteins > cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Page last updated: 2024-08-07 13:49:24
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
A cAMP and cAMP-inhibited cGMP 3,5-cyclic phosphodiesterase 10A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y233]
Synonyms
EC 3.1.4.17;
EC 3.1.4.35
Research
Bioassay Publications (36)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (19.44) | 29.6817 |
| 2010's | 24 (66.67) | 24.3611 |
| 2020's | 5 (13.89) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dipyridamole | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| papaverine | Homo sapiens (human) | IC50 | 0.0700 | 12 | 13 |
| rolipram | Homo sapiens (human) | IC50 | 141.6064 | 2 | 11 |
| zardaverine | Homo sapiens (human) | IC50 | 99.7820 | 1 | 10 |
| papaverine hydrochloride | Homo sapiens (human) | IC50 | 1.6191 | 2 | 2 |
| 5-nitroquinoline | Homo sapiens (human) | Ki | 590.0000 | 1 | 1 |
| 2-amino-4,6-dimethyl pyrimidine | Homo sapiens (human) | Ki | 1,300.0000 | 1 | 1 |
| 5-nitroindazole | Homo sapiens (human) | Ki | 560.0000 | 1 | 1 |
| 7-chloro-4-hydroxyquinoline | Homo sapiens (human) | Ki | 500.0000 | 1 | 1 |
| tadalafil | Homo sapiens (human) | IC50 | 68.0807 | 5 | 15 |
| 9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| cilomilast | Homo sapiens (human) | IC50 | 50.2760 | 1 | 11 |
| rp 73401 | Homo sapiens (human) | IC50 | 36.7900 | 1 | 10 |
| 2-amino-4-methyl-3-nitropyridine | Homo sapiens (human) | Ki | 300.0000 | 1 | 1 |
| vinpocetine | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| roflumilast | Homo sapiens (human) | IC50 | 124.2002 | 1 | 10 |
| sch 351591 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| pf-2545920 | Homo sapiens (human) | IC50 | 0.0013 | 9 | 9 |
| pf 04217903 | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| 3-(2,5-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine | Homo sapiens (human) | IC50 | 0.8230 | 1 | 1 |
| azd7687 | Homo sapiens (human) | IC50 | 5.5000 | 1 | 1 |
| an2728 | Homo sapiens (human) | IC50 | 97,600.0000 | 1 | 1 |
| sildenafil | Homo sapiens (human) | IC50 | 27.4468 | 6 | 15 |
| zaprinast | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| vardenafil | Homo sapiens (human) | IC50 | 6.1142 | 3 | 12 |
| 2-methyl-4(3h)-quinazolinone | Homo sapiens (human) | Ki | 990.0000 | 1 | 1 |
| 4-hydroxyquinazoline | Homo sapiens (human) | Ki | 910.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| cinchophen | Homo sapiens (human) | Kd | 127.0000 | 1 | 1 |
| oxycinchophen | Homo sapiens (human) | Kd | 15.0000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| papaverine | Homo sapiens (human) | IC20 | 0.6500 | 1 | 1 |
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
Why All the Fuss about Oxidative Phosphorylation (OXPHOS)?Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 29, Issue:11, 2019
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 25, Issue:4, 2015
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.Bioorganic & medicinal chemistry, , May-01, Volume: 22, Issue:9, 2014
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 21, Issue:19, 2013
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 22, Issue:5, 2012
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
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 imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
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
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 25, Issue:4, 2015
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.Bioorganic & medicinal chemistry, , May-01, Volume: 22, Issue:9, 2014
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 21, Issue:19, 2013
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
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
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
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 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
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] |
| cGMP-stimulated cyclic-nucleotide phosphodiesterase activity | molecular function | Catalysis of the reaction: nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate; catalytic activity is increased in the presence of cGMP. [GOC:mah] |
| cAMP binding | molecular function | Binding to cAMP, the nucleotide cyclic AMP (adenosine 3',5'-cyclophosphate). [GOC:ai] |
| 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-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
| 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 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] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| cAMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of the nucleotide cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate). [ISBN:0198506732] |
| cGMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of cyclic GMP, guanosine 3',5'-phosphate. [GOC:go_curators] |
| negative regulation of cGMP-mediated signaling | biological process | Any process that decreases the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, 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] |