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138 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28686445 39 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.EBI Sun Yat-sen University
28406621 65 Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.EBI Dart Neuroscience LLC
28165743 37 Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.EBI Dart Neuroscience LLC
27597413 58 Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.EBI Southern Medical University
27301679 21 Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket.EBI Takeda Pharmaceutical Co., Ltd
26978121 20 Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.EBI Sun Yat-sen University
26789933 100 Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.EBI Intra-Cellular Therapies Inc
26935942 41 Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.EBI Mercachem
26562545 13 Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and inávitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.EBI Institute of Radiopharmaceutical Cancer Research
26421921 43 Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.EBI Glenmark Research Centre
26526739 35 Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.EBI Southern Medical University
26494583 8 Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.EBI Takeda Pharmaceutical Co., Ltd
26430878 102 Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.EBI Washington University
26077491 31 Discovery of [╣╣C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.EBI Merck Research Laboratories
26378882 45 Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.EBI Merck Research Laboratories
25592707 31 Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.EBI Washington University
26113188 9 BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.EBI University of Copenhagen
25801159 36 Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.EBI CSIR-Indian Institute of Integrative Medicine
25630223 5 Target engagement in lead generation.EBI Eli Lilly and Company
25016376 13 Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.EBI Universit£ di Sassari
24980052 37 Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.EBI Glenmark Pharmaceuticals Ltd
25456383 113 Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.EBI TBA
25432025 34 Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.EBI Sun Yat-sen University
24944747 18 Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).EBI Amgen Inc
24837154 18 Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.EBI Yamanouchi Pharmaceutical Co., Ltd
24725435 15 Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.EBI Glenmark Pharmaceuticals Ltd
24721831 2 Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.EBI Washington University
23509991 23 Development of a plate-based optical biosensor fragment screening methodology to identify phosphodiesterase 10A inhibitors.EBI AstraZeneca
24900650 3 PDE10 Inhibitors as Potential Treatment for Schizophrenia.EBI Therachem Research Medilab (India) Pvt. Ltd.
23260348 91 Discovery of a new series of [1,2,4]triazolo[4,3-a]quinoxalines as dual phosphodiesterase 2/phosphodiesterase 10 (PDE2/PDE10) inhibitors.EBI Janssen-Cilag S.A.
23149228 60 Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.EBI Amgen Inc
22892116 30 Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI Merck Research Laboratories
23137303 38 Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.EBI Chinese Academy of Sciences
23116186 68 Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).EBI AstraZeneca
22985069 18 Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.EBI Sun Yat-sen University
22834877 119 Current landscape of phosphodiesterase 10A (PDE10A) inhibition.EBI Pfizer Inc
22902656 42 Novel triazines as potent and selective phosphodiesterase 10A inhibitors.EBI Pfizer Inc
22548439 9 Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.EBI Amgen Inc
22377514 75 The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI Merck Research Laboratories
18299198 73 CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors.EBI St. John's University
15887951 29 The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.EBI Monash University (Parkville Campus)
22365755 42 Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.EBI Amgen Inc
22321214 42 Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.EBI AstraZeneca
22227212 58 Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.EBI Merck Research Laboratories
22222034 35 The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.EBI Merck Research Laboratories
22142545 96 Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.EBI Merck Research Laboratories
21988093 316 Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.EBI Pfizer Inc
21983442 142 Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.EBI BioCrea GmbH
21705115 37 Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.EBI Washington University
21602043 50 Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.EBI H. Lundbeck A/S
21087867 30 Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.EBI Universit£ di Sassari
20450197 80 Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.EBI Biotie Therapies GmbH
19919087 55 Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.EBI Pfizer Inc
17683932 55 Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.EBI Schering-Plough Research Institute
17400452 42 PDE-10A inhibitors as insulin secretagogues.EBI Bayer Pharmaceuticals Corporation
16275071 26 A new chemical tool for exploring the physiological function of the PDE2 isozyme.EBI Pfizer Inc
16263279 37 A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.EBI Pfizer Inc
15837326 51 Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.EBI Schering-Plough Research Institute
26602277 42 Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI Merck Research Laboratories
26597534 14 Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.EBI AstraZeneca
25062128 16 Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).EBI Amgen Inc.
23585921 52 Synthesis and EBI Washington University School of Medicine
24231362 13 Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors.EBI Glenmark Pharmaceuticals Limited
24102193 17 Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).EBI Amgen Inc.
23978358 28 N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.EBI H. Lundbeck A/S
30245400 167 Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.EBI Shandong University
30258530 6 Potential of PDE10A Inhibitors as Treatment for Schizophrenia and Other Neurological Disorders.EBI Therachem Research Medilab, LLC.
30148362 36 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.EBI Sun Yat-Sen University
29545101 55 Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.EBI South China Agricultural University
29870883 106 Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.EBI Celon Pharma S.A.
29291443 30 Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.EBI Sun Yat-sen University
29718668 27 Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.EBI Pfizer Inc
28796496 67 Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.EBI Takeda Pharmaceutical Co., Ltd
28759228 36 Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.EBI Takeda Pharmaceutical Co., Ltd
29200281 20 Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.EBI Chiesi Farmaceutici S.p.A.
28800229 2 Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors.EBI IOTA Pharmaceuticals
28462841 26 Design and optimization of purine derivatives as in vivo active PDE10A inhibitors.EBI Nanchang University
22225576 11 Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide.BDB Umeň University
21999604 43 Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds.BDB Ondokuz Mayis University
21171894 6 Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.BDB Bristol-Myers Squibb Co.
28166391 18 Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair.BDB UniversitÚ de Nantes
23737523 3 The chlorite dismutase (HemQ) from Staphylococcus aureus has a redox-sensitive heme and is associated with the small colony variant phenotype.BDB University of Notre Dame
10411588 4 Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.BDB The University of Calgary
15850980 12 Switching between allosteric and dimerization inhibition of HIV-1 protease.BDB Purdue University
18242982 38 Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.BDB Bristol-Myers Squibb Co.
18278855 13 Exploring inhibitor binding at the s' subsites of cathepsin L.BDB National Research Council Canada
17174550 26 Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.BDB Bristol-Myers Squibb Co.
14998322 3 Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.BDB Morphochem AG
17083960 39 Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.BDB Medical College of Wiscosin
16046538 84 Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.BDB Ambit, Inc.
16203148 15 Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.BDB Merck Research Laboratories
8978850 205 Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.BDB Sphinx Laboratories
9703473 207 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.BDB Parke-Davis Pharmaceutical Research
10821714 29 Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.BDB DuPont Pharmaceuticals Company
7684450 26 Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a BDB Upjohn