106 articles for thisTarget
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Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.
Vertex Pharmaceuticals
Benzimidazole-containing HCV NS5A inhibitors: effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency.
Vertex Pharmaceuticals
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.
Vertex Pharmaceuticals
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.
Vertex Pharmaceuticals
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Vertex Pharmaceuticals
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors.
Vertex Pharmaceuticals
Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: non-symmetric inhibitors with potent activity against genotype 1a and 1b.
Vertex Pharmaceuticals
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Vertex Pharmaceuticals
Strategies for the modulation of phase II metabolism in a series of PKCe inhibitors.
Vertex Pharmaceuticals
Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase¿.
Vertex Pharmaceuticals
Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator.
Vertex Pharmaceuticals
Identification of novel HSP90a/ß isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Vertex Pharmaceuticals
Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Vertex Pharmaceuticals
Correlation between chemotype-dependent binding conformations of HSP90a/ß and isoform selectivity-Implications for the structure-based design of HSP90a/ß selective inhibitors for treating neurodegenerative diseases.
Vertex Pharmaceuticals
Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.
Vertex Pharmaceuticals
Structure-based optimization of aminopyridines as PKC¿ inhibitors.
Vertex Pharmaceuticals
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides.
Vertex Pharmaceuticals
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Vertex Pharmaceuticals
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
Vertex Pharmaceuticals
Discovery and development of aurora kinase inhibitors as anticancer agents.
Vertex Pharmaceuticals
Kinase-likeness and kinase-privileged fragments: toward virtual polypharmacology.
Vertex Pharmaceuticals
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Vertex Pharmaceuticals
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.
Vertex Pharmaceuticals
Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.
Vertex Pharmaceuticals
4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.
Vertex Pharmaceuticals
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.
Vertex Pharmaceuticals
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Vertex Pharmaceuticals
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.
Vertex Pharmaceuticals
Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.
Vertex Pharmaceuticals
Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).
Vertex Pharmaceuticals
Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2.
Vertex Pharmaceuticals
Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates.
Vertex Pharmaceuticals
Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.
Vertex Pharmaceuticals
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Vertex Pharmaceuticals
BREED: Generating novel inhibitors through hybridization of known ligands. Application to CDK2, p38, and HIV protease.
Vertex Pharmaceuticals
Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.
Vertex Pharmaceuticals
Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.
Vertex Pharmaceuticals
Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants.
Vertex Pharmaceuticals
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Vertex Pharmaceuticals
A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors.
Vertex Pharmaceuticals
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
Discovery of Novel Thiophene-Based, Thumb Pocket 2 Allosteric Inhibitors of the Hepatitis C NS5B Polymerase with Improved Potency and Physicochemical Profiles.
Vertex Pharmaceuticals
Fragment-Based Discovery of Dual JC Virus and BK Virus Helicase Inhibitors.
Vertex Pharmaceuticals
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Vertex Pharmaceuticals
Synthesis of a 6-Aza-Isoindolinone-Based Inhibitor of Phosphoinositide 3-Kinase γ via Ruthenium-Catalyzed [2 + 2 + 2] Cyclotrimerization.
Vertex Pharmaceuticals
Design and synthesis of novel conformationally restricted HIV protease inhibitors.
Vertex Pharmaceuticals
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
Vertex Pharmaceuticals
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Vertex Pharmaceuticals
Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease.
Vertex Pharmaceuticals
Phenotypic and structural analyses of hepatitis C virus NS3 protease Arg155 variants: sensitivity to telaprevir (VX-950) and interferon alpha.
Vertex Pharmaceuticals
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.
Vertex Pharmaceuticals
Are free energy calculations useful in practice? A comparison with rapid scoring functions for the p38 MAP kinase protein system.
Vertex Pharmaceuticals
ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Vertex Pharmaceuticals
ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Vertex Pharmaceuticals
Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions.
Vertex Pharmaceuticals
Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinaseγ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).
Vertex Pharmaceuticals
INHIBITORS OF SPINSTER HOMOLOG 2 (SPNS2) FOR USE IN THERAPY
University of Virginia Patent Foundation
Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
Shionogi
Biaryl derivative, preparation method thereof and pharmaceutical application thereof
Abbisko Therapeutics
Substituted benzimidazoles, their preparation and their use as pharmaceuticals
Epigenetix
Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy
The Johns Hopkins University
Compositions and methods to modulate chloride ion channel activity
The Leland Stanford Junior University
Tetrahydroisoquinolines and terahydronaphthyridines for the treatment of hepatitis B virus infection
Hoffmann-La Roche
Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders
AchÉ
Compositions and methods for treating disorders of circadian and diurnal rhythms using prokineticin 2 agonists and antagonists
University of California
Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases
Biogen Ma
CARBOXYLIC ACID AROMATIC AMIDES AS ANTAGONISTS OF BRADYKININ B1 RECEPTOR
Bayer Pharma Aktiengesellschaft
Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase
North Carolina Central University
Sydnonimines-specific dopamine reuptake inhibitors and their use in treating dopamine related disorders
Caliper Life Sciences
Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-α]pyrazine-2-carboxamides as RSK inhibitors
Phoenix Molecular Designs
Pyrrolo[2,3-C]pyridines as imaging agents for neurofibrilary tangles
Merck Sharp & Dohme
Potent and Selective EphA4 Agonists for the Treatment of ALS.
Sanford Burnham Prebys Medical Discovery Institute
Insights into distinct modulation of a7 and a7ß2 nicotinic acetylcholine receptors by the volatile anesthetic isoflurane.
University of Pittsburgh
Naphthalene-based inhibitors of anti-apoptotic proteins
Burnham Institute For Medical Research
Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.
Tehran University of Medical Sciences
Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.
Universit&Aagrove
Pharmacological characterization of cloned chicken neuropeptide Y receptors Y1 and Y5.
Uppsala University
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors.
Georgetown University
Differential expression of multiple somatostatin receptors in the rat cerebellum during development.
Dynamique Des Systemes Neuroendocriniens
Pharmacological properties of recombinant "diazepam-insensitive" GABAA receptors.
National Institute of Diabetes, Digestive and Kidney Diseases
Structural determinants of inhibitor selectivity in prokaryotic IMP dehydrogenases.
Brandeis University
Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.
Pfizer
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
Incyte
Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles.
Wyeth Research