218 articles for thisTarget
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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with
Merck
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Merck Research Laboratories
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Merck
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Merck
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Xenon Pharmaceuticals
Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.
Amgen
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Merck Research Laboratories
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Daiichi Sankyo
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
Merck Research Laboratories
Bioavailable pyrrolo-benzo-1,4-diazines as Na(v)1.7 sodium channel blockers for the treatment of pain.
Merck Research Laboratory
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
Astrazeneca
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Pfizer
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Prediction of Thorough QT study results using action potential simulations based on ion channel screens.
University of Oxford
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
University of Oxford
Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Amgen
Discovery of pyrrolo-benzo-1,4-diazines as potent Na(v)1.7 sodium channel blockers.
Merck Research Laboratory
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.
Astrazeneca
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.
Xenon Pharmaceuticals
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Astrazeneca
Imidazol-1-ylethylindazole voltage-gated sodium channel ligands are neuroprotective during optic neuritis in a mouse model of multiple sclerosis.
University College London
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.
Astrazeneca
Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship.
Astrazeneca
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
Lead optimization of antimalarial propafenone analogues.
St. Jude Children'S Research Hospital
Phenethyl nicotinamides, a novel class of Na(V)1.7 channel blockers: structure and activity relationship.
Astrazeneca
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.
Astrazeneca
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
TBA
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Merck Research Laboratories
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
University of Bari Aldo Moro
Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.
Amgen
The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.
Amgen
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Merck Research Laboratories
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Abbott Laboratories
Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation.
Cardiome Pharma
4,5-Dihydro-3-(methanesulfonamidophenyl)-1-phenyl-1H-2,4-benzodiazepines: a novel class III antiarrhythmic agents.
Sterling Winthrop Research
Asymmetric synthesis and evaluation of a hydroxyphenylamide voltage-gated sodium channel blocker in human prostate cancer xenografts.
University of Virginia
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Amgen
Lactam-stabilized helical analogues of the analgesicµ-conotoxin KIIIA.
Monash University
Optimization of propafenone analogues as antimalarial leads.
St. Jude Children'S Research Hospital
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Merck
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Merck Frosst Centre For Therapeutic Research
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Merck Research Laboratories
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Abbott Laboratories
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Wyeth Research
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
Pfizer
Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.
Astrazeneca R & D M£Lndal
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Merck Research Laboratories
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Merck Research Laboratories
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
Pierre Fabre Research Center
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Abbott Laboratories
Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.
University of Utah
A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.
Johns Hopkins University
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
University of Cambridge
New aryl and acylsulfonamides as state-dependent inhibitors of Nav1.3 voltage-gated sodium channel.
University of Ljubljana
α-Fluorination of tropane compounds and its impact on physicochemical and ADME properties.
Eisai Co., Ltd.
Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure-Activity Relationships.
Merck & Co.
2-Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model.
Merck & Co.
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
University of Kentucky
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Biogen Research and Development
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease.
Merck
Discovery of a Novel Ketohexokinase Inhibitor with Improved Drug Distribution in Target Tissue for the Treatment of Fructose Metabolic Disease.
Tuojie Biotech (Shanghai) Co.
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
Merck
Optimization of the Antibacterial Spectrum and the Developability Profile of the Novel-Class Natural Product Corramycin.
Evotec
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Pfizer
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Merck
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (Na
Xenon Pharmaceuticals
Design, synthesis, and biological evaluation of acyl sulfonamide derivatives with spiro cycles as Na
Fudan University
The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders.
Sosei Heptares
Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation.
Novartis Institutes For Biomedical Research
Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.
IRBM Science Park
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS
Novartis Institutes For Biomedical Research
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
University College London
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.
Peking Union Medical College
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na
Abbvie
Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β
Chiesi Farmaceutici
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
Wuxi Apptec
Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
Wuxi Apptec
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of
Ucb
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Merck
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Biogen
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.
Merck
Functional Characterization of the Nemertide α Family of Peptide Toxins.
Uppsala University
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Merck
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Merck
Identification of aryl sulfonamides as novel and potent inhibitors of Na
Xenon Pharmaceuticals
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Novartis Institutes For Biomedical Research
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.
University of Wollongong
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Sareum
Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2.
Redx Anti-Infectives
Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Cenes Pharmaceuticals
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
University of Washington
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
Amgen
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure.
Merck Research Laboratories
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.
Recordati
Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.
Goldfinch Bio
Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease.
TBA
Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.
Astrazeneca
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.
The Walter and Eliza Hall Institute of Medical Research
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na
Bristol-Myers Squibb Research and Development
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Merck
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Glaxosmithkline
Discovery of new indole-based acylsulfonamide Na
Bristol-Myers Squibb Research and Development
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.
Merck
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
Siteone Therapeutics
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.
Merck
Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2-aminoimidazoles as voltage-gated sodium channel modulators.
University of Ljubljana
Novel state-dependent voltage-gated sodium channel modulators, based on marine alkaloids from Agelas sponges.
University of Ljubljana
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.
Trevena
Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507.
Astrazeneca
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Merck
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Merck
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.
Pfizer
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa
Xenon Pharmaceuticals
Discovery of morpholine-based aryl sulfonamides as Na
Bristol-Myers Squibb Research and Development
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Idorsia Pharmaceuticals
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
Wuxi Apptec (Shanghai)
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.
Glaxosmithkline
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Daiichi Sankyo
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na
Amgen
Discovery of non-zwitterionic aryl sulfonamides as Na
Bristol-Myers Squibb Research and Development
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)
Sage Therapeutics
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na
Icagen
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Vanderbilt University Institute of Imaging Science
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Merck
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department of Discovery Chemistry Merck
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.
Wuxi Apptec (Shanghai)
Fused ring compound having urea structure
Sanford Burnham Prebys Medical Discovery Institute
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors
Eli Lilly
Thienodiazepine derivatives and application thereof
Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang)
Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Tetrahydroacridine derivatives with fluorobenzoic acid moiety as multifunctional agents for Alzheimer's disease treatment.
Medical University of Lodz
Substituted 3-haloallylamine inhibitors of ASSAO and uses thereof
Boehringer Ingelheim International
Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors
Pharmacyclics
Characterization of MymA protein as a flavin-containing monooxygenase and as a target of isoniazid.
Miranda House
3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.
Jilin University
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.
University of Wisconsin-Madison
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors.
Eli Lilly
Synthesis, kinetic evaluation and cell-based analysis of C-alkylated isofagomines as chaperones of β-glucocerebrosidase.
University of British Columbia
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.
Abbott Laboratories
An alternative purification method for human serum paraoxonase 1 and its interactions with sulfonamides.
Ataturk University
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
Array Biopharma