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159 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
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
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.EBI
Dart Neuroscience
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.EBI
Dart Neuroscience
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
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
Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.EBI
Sun Yat-Sen University
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
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.EBI
Mercachem
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.EBI
Institute Of Radiopharmaceutical Cancer Research
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.EBI
Glenmark Research Centre
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.EBI
Southern Medical University
Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.EBI
Takeda Pharmaceutical
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
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.EBI
Merck Research Laboratories
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
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.EBI
Washington University
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.EBI
University Of Copenhagen
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.EBI
Csir-Indian Institute Of Integrative Medicine
Target engagement in lead generation.EBI
Eli Lilly
Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.EBI
Universit£
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.EBI
Glenmark Pharmaceuticals
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.EBI
TBA
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.EBI
Sun Yat-Sen University
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).EBI
Amgen
Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.EBI
Yamanouchi Pharmaceutical
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.EBI
Glenmark Pharmaceuticals
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.EBI
Washington University
Development of a plate-based optical biosensor fragment screening methodology to identify phosphodiesterase 10A inhibitors.EBI
Astrazeneca
PDE10 Inhibitors as Potential Treatment for Schizophrenia.EBI
Therachem Research Medilab (India)
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
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.EBI
Amgen
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI
Merck Research Laboratories
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.EBI
Chinese Academy Of Sciences
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).EBI
Astrazeneca
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.EBI
Sun Yat-Sen University
Current landscape of phosphodiesterase 10A (PDE10A) inhibition.EBI
Pfizer
Novel triazines as potent and selective phosphodiesterase 10A inhibitors.EBI
Pfizer
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.EBI
Amgen
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI
Merck Research Laboratories
CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors.EBI
St. John'S University
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.EBI
Monash University (Parkville Campus)
Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.EBI
Amgen
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.EBI
Astrazeneca
Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.EBI
Merck Research Laboratories
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.EBI
Merck Research Laboratories
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.EBI
Merck Research Laboratories
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.EBI
Pfizer
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.EBI
Biocrea
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.EBI
Washington University
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.EBI
H. Lundbeck
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.EBI
Universit£
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.EBI
Biotie Therapies
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.EBI
Pfizer
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.EBI
Schering-Plough Research Institute
PDE-10A inhibitors as insulin secretagogues.EBI
Bayer Pharmaceuticals
A new chemical tool for exploring the physiological function of the PDE2 isozyme.EBI
Pfizer
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.EBI
Pfizer
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
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.EBI
Janssen Research & Development
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.EBI
Vrije Universiteit Amsterdam
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.EBI
Palack£
Absolute Binding Free Energy Calculation and Design of a Subnanomolar Inhibitor of Phosphodiesterase-10.EBI
Sun Yat-Sen University
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.EBI
Guangzhou University Of Chinese Medicine
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.EBI
Shanghai Institute Of Materia Medica
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.EBI
Chinese Academy Of Sciences
Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors.EBI
Astellas Pharma
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.EBI
Sun Yat-Sen University
Fragment-to-Lead Medicinal Chemistry Publications in 2018.EBI
Frontier Medicines
Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.EBI
Abbvie Deutschland
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.EBI
Changzhou University
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.EBI
Sun Yat-Sen University
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.EBI
Mitsubishi Tanabe Pharma
Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability.EBI
TBA
Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.EBI
Asubio Pharma
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.EBI
South China Agricultural University
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.EBI
Merck Research Laboratories
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.EBI
Astrazeneca
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
Synthesis and EBI
Washington University School Of Medicine
Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors.EBI
Glenmark Pharmaceuticals
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).EBI
Amgen
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.EBI
H. Lundbeck
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.EBI
Shandong University
Potential of PDE10A Inhibitors as Treatment for Schizophrenia and Other Neurological Disorders.EBI
Therachem Research Medilab
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
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.EBI
South China Agricultural University
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.EBI
Celon Pharma
Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.EBI
Sun Yat-Sen University
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.EBI
Pfizer
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
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.EBI
Takeda Pharmaceutical
Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.EBI
Chiesi Farmaceutici
Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors.EBI
Iota Pharmaceuticals
Design and optimization of purine derivatives as in vivo active PDE10A inhibitors.EBI
Nanchang University
Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide.BDB
Umeå University
Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds.BDB
Ondokuz Mayis University
Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.BDB
Bristol-Myers Squibb
Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair.BDB
Universit?? De Nantes
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
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
Switching between allosteric and dimerization inhibition of HIV-1 protease.BDB
Purdue University
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
Exploring inhibitor binding at the s' subsites of cathepsin L.BDB
National Research Council Canada
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.BDB
Bristol-Myers Squibb
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.BDB
Morphochem
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.BDB
Medical College Of Wiscosin
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.BDB
Ambit
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.BDB
Merck Research Laboratories
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
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
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.BDB
Dupont Pharmaceuticals
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