125 articles for thisTarget
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Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X
The University of Sydney
Escape from adamantane: Scaffold optimization of novel P2X7 antagonists featuring complex polycycles.
Universitat De Barcelona
The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.
Janssen Research and Development
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Janssen Research and Development
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.
Janssen Research and Development
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.
Janssen Research and Development
Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.
University of Leeds
Discovery of novel 2,5-dioxoimidazolidine-based P2X(7) receptor antagonists as constrained analogues of KN62.
Gwangju Institute of Science and Technology (Gist)
Design and synthesis of potent and selective P2X3 receptor antagonists derived from PPADS as potential pain modulators.
Gwangju Institute of Science and Technology (Gist)
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
University of Cambridge
Synthesis and structure-activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists.
Gwangju Institute of Science and Technology
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Janssen Research and Development
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Abbott Laboratories
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
Abbott Laboratories
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Glaxosmithkline
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Glaxosmithkline
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.
Roche Palo Alto
Antagonists of the P2X(7) receptor. From lead identification to drug development.
Astrazeneca
Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.
Abbott Laboratories
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Abbott Laboratories
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Abbott Laboratories
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Abbott Laboratories
N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.
University of Bonn
Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.
Gwangju Institute of Science and Technology (Gist)
Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.
University of Bonn
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
Abbott Bioresearch Center
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.
Astrazeneca R&D Charnwood
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2.
Merck Research Laboratories
Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor.
Pfizer
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.
Glaxosmithkline
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.
Merck Research Laboratories
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Pfizer
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.
Pfizer
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.
Institute of Science & Technology
Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening.
University of Sydney
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Roche Palo Alto
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Roche Palo Alto
Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists.
Institute of Science and Technology (Gist)
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Abbott Bioresearch Center
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.
Institute of Science and Technology
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
Astrazeneca R&D Charnwood
From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.
Università
Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury.
Sichuan University
From lead to clinic: A review of the structural design of P2X7R antagonists.
Sichuan University
Exploratory study of oxatomide derivatives with high P2X
Takasaki University of Health and Welfare
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Therapeutic potentials and structure-activity relationship of 1,3-benzodioxole N-carbamothioyl carboxamide derivatives as selective and potent antagonists of P2X4 and P2X7 receptors.
Comsats University Islamabad
Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.
Comsats University Islamabad
Unveiling the Structure-Activity Relationships at the Orthosteric Binding Site of P2X Ion Channels: The Route to Selectivity.
European Institute For Molecular Imaging (Eimi)
Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.
Yeditepe University
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Lundbeck Research Usa
Discovery of bilirubin as novel P2X7R antagonist with anti-tumor activity.
Zhengzhou University
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.
Università
Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists.
European Institute For Molecular Imaging (Eimi)
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Shionogi
Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.
Università
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
Universidad Aut£Noma De Madrid
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
University of Lille
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
University of Bonn
Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion.
Gwangju Institute of Science and Technology (Gist)
The evolution of P2X7 antagonists with a focus on CNS indications.
Janssen Pharmaceutical Research & Development
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Shionogi
Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.
Università
Development of High-Throughput Fluorescent-Based Screens to Accelerate Discovery of P2X Inhibitors from Animal Venoms.
University of East Anglia
8-Hydroxy-2-(1H-1,2,3-triazol-1-yl)-1,4-naphtoquinone derivatives inhibited P2X7 Receptor-Induced dye uptake into murine Macrophages.
Fluminense Federal University
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists.
Emd Serono Research and Development Institute
Synthesis and in vitro biological evaluation of new P2X7R radioligands [
Indiana University School of Medicine
Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.
Gwangju Institute of Science and Technology (Gist)
Purinergic receptor P2X₇: a novel target for anti-inflammatory therapy.
Punjabi University
Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.
Gwangju Institute of Science and Technology (Gist)
1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
Instituto De Tecnologia Em F£Rmacos
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.
Shionogi
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Janssen Research and Development
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Janssen Research and Development
Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X
The University of Sydney
Composition and methods for inhibiting mammalian sterile 20-like kinase 1
The Scripps Research Institute
[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11BH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto
Neurocrine Biosciences
Methods to determine KDM1A target engagement and chemoprobes useful therefor
Oryzon Genomics
Potent Noncovalent Inhibitors of the Main Protease of SARS-CoV-2 from Molecular Sculpting of the Drug Perampanel Guided by Free Energy Perturbation Calculations
Yale University
Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
Abbvie
Piperazine-substituted benzothiophenes for treatment of mental disorders
Otsuka Pharmaceutical
The synthesis of novel pyrazole-3,4-dicarboxamides bearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II.
Dumlupinar University
2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
Merck Sharp & Dohme
Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions.
Aston University
Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin
The Procter & Gamble
Method of treating human skin and a skin care composition for use in such a method
Pantarhei Bioscience
Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.
University of North Carolina At Chapel Hill
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
University of California Berkeley
[1,3,4] oxadiazole derivative and application thereof
Huazhong University of Science & Technology
Thermodynamics of binding of structurally similar ligands to histone deacetylase 8 sheds light on challenges in the rational design of potent and isozyme-selective inhibitors of the enzyme.
North Dakota State University
Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as cFMS inhibitors
Array Biopharma
Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors.
Jiangnan University
Preparation of triazole-linked glycosylated ??????-ketocarboxylic acid derivatives as new PTP1B inhibitors.
East China University of Science and Technology
Hydrolytic mechanism of OXA-58 enzyme, a carbapenem-hydrolyzing class D β-lactamase from Acinetobacter baumannii.
York University
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
Albany Medical College
Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Novartis Pharma
Comparison of the pharmacological properties of cloned rat, human, and bovine norepinephrine transporters.
The University of Queensland