58 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.
Actelion Pharmaceuticals
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
Actelion Pharmaceuticals
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups.
Actelion Pharmaceuticals
Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines.
Actelion Pharmaceuticals
Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.
Actelion Pharmaceuticals
Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.
Actelion Pharmaceuticals
Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation.
Actelion Pharmaceuticals
Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.
Actelion Pharmaceuticals
Novel S1P1 receptor agonists--part 1: From pyrazoles to thiophenes.
Actelion Pharmaceuticals
Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity.
Actelion Pharmaceuticals
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.
Actelion Pharmaceuticals
Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold.
Actelion Pharmaceuticals
Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist.
Actelion Pharmaceuticals
Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.
Actelion Pharmaceuticals
Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity.
Actelion Pharmaceuticals
The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.
Actelion Pharmaceuticals
Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.
Actelion Pharmaceuticals
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.
Actelion Pharmaceuticals
Design and optimization of new piperidines as renin inhibitors.
Actelion Pharmaceuticals
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Actelion Pharmaceuticals
Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.
Actelion Pharmaceuticals
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.
Actelion Pharmaceuticals
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
Actelion Pharmaceuticals
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Actelion Pharmaceuticals
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.
Actelion Pharmaceuticals
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Actelion Pharmaceuticals
Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines.
Actelion Pharmaceuticals
Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes.
Actelion Pharmaceuticals
Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria.
Actelion Pharmaceuticals
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
Actelion Pharmaceuticals
Pyrimidinyl group-containing tricyclic compound serving as c-Met inhibitor
Jiangsu Aosaikang Pharmaceutical
Ligand Discovery for a Peptide-Binding GPCR by Structure-Based Screening of Fragment- and Lead-Like Chemical Libraries.
Stockholm University
The SAMPL4 host-guest blind prediction challenge: an overview.
University of California San Diego
Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
Johannes Gutenberg—Universitat Mainz
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
Molecular Basis of 1-Deoxygalactonojirimycin Arylthiourea Binding to Human a-Galactosidase A: Pharmacological Chaperoning Efficacy on Fabry Disease Mutants.
Tottori University , Yonago 683-8503, Japan
Nature of the active site of a subunit of the first component of human complement.
Michigan State University
Identification and Characterization of Small Molecule Inhibitors of a Plant Homeodomain Finger.
University of Wisconsin
Hydrolytic mechanism of OXA-58 enzyme, a carbapenem-hydrolyzing class D β-lactamase from Acinetobacter baumannii.
York University
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.
Institut De Recherches Servier
Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor.
Taisho Pharmaceutical
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.
The University of Calgary
A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms.
The Scripps Research Institute