235 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.
Glaxosmithkline
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole.
Pfizer
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Bristol-Myers Squibb
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists.
Bristol-Myers Squibb Research and Development
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.
National Institute of Biological Sciences, Beijing
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
Yonsei University
Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors.
University of Illinois At Chicago
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Glaxosmithkline
Derivatives of dibenzothiophene for positron emission tomography imaging ofa7-nicotinic acetylcholine receptors.
The Johns Hopkins University School of Medicine
5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): a novel non-nitrogenous ligand for 5-HT2B receptor.
Virginia Commonwealth University
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
University of Missouri
Design of fluorinated 5-HT(4)R antagonists: influence of the basicity and lipophilicity toward the 5-HT(4)R binding affinities.
University of Southampton
Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.
University of Modena and Reggio Emilia
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
National Institute of Mental Health
In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.
University of Mississippi
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.
Virginia Commonwealth University
Discovery of ML314, a Brain Penetrant Non-Peptidicβ-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Sanford-Burnham Medical Research Institute
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.
Theravance
Selectivity of phenothiazine cholinesterase inhibitors for neurotransmitter systems.
Dalhousie University
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School of Pharmacy
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists.
Bristol-Myers Squibb Pharmaceutical Research Institute
Near native binding of a fluorescent serotonin conjugate to serotonin type 3 receptors.
Washington State University
Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine.
TBA
Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789).
Siena Biotech
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A.
Vu University Amsterdam
Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.
University of Modena and Reggio Emilia
Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.
Glaxosmithkline
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
Merck Sharp & Dohme Research Laboratories
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.
Savannah State University
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
Discovery of (2S,3R)-N-[2-(Pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selectivea7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.
Targacept
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.
University of Caen Normandie
N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward ana7 nicotinic acetylcholine receptor agonist preclinical candidate.
Siena Biotech
Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.
Suven Life Sciences
Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selectivea4ß2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Targacept
Design, synthesis, and structure-activity relationships of highly potent 5-HT3 receptor ligands.
Vu University Amsterdam
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
University of Namur
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.
University of Warwick
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).
Sepracor
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
European Research Centre For Drug Discovery and Development (Natsyndrugs)
A comprehensive study on the 5-hydroxytryptamine(3A) receptor binding of agonists serotonin and m-chlorophenylbiguanidine.
Virtua Drug
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
Pfizer
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.
Purdue University
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
Pfizer
An antidepressant that extends lifespan in adult Caenorhabditis elegans.
Howard Hughes Medical Institute
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.
F. Hoffmann-La Roche
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
F. Hoffmann-La Roche
Multi-target-directed ligands to combat neurodegenerative diseases.
University of Bologna
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
University of Copenhagen
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
University of Urbino
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
Alcon Research
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
Virginia Commonwealth University
Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties.
Universidad Complutense
An initial three-component pharmacophore for specific serotonin-3 receptor ligands.
Pfizer
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Pfizer
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
University of Florida
New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor
TBA
Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H3 receptor antagonists with potent cognition enhancing activity.
Cephalon
New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.
Universidad Complutense De Madrid
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features.
Abbott Healthcare Products
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Pfizer
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
Amri
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Purdue University
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Siena Biotech
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
Meiji Seika Kaisha
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
Pfizer
Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.
Hungarian Academy of Sciences
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.
Pfizer
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.
TBA
(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor
TBA
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists
TBA
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
European Research Centre For Drug Discovery and Development (Natsyndrugs)
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Pfizer
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
Université
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
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Novartis Institutes For Biomedical Research
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
Washington University
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Uppsala University
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Inhibitors of unactivated p38 MAP kinase.
Johnson and Johnson Pharmaceutical Research and Development
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Merck
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
University College London
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Carlsson Research
Discovery of G Protein-Biased Ligands against 5-HT
Korea Institute of Science and Technology
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives as potential SSRIs.
Sunshine Lake Pharma
Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
Sunshine Lake Pharma
Discovery of G Protein-Biased Antagonists against 5-HT
Korea Institute of Science and Technology
Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.
Sungkyunkwan University
Development of a presynaptic 5-HT1A antagonist.
Bristol-Myers Squibb Pharmaceutical Research Institute
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
The University of Louisiana At Monroe
New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants.
Universidad De Navarra
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Virginia Commonwealth University
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Discovery of fused heterocyclic carboxamide derivatives as novel α7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation.
Peking University
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
Knoll Pharmaceuticals
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.
Rti International
Bis(het)aryl-1,2,3-triazole quinuclidines as α7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [
Orleans University
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
Merck Sharp and Dohme Research Laboratories
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.
Yamanouchi Pharmaceutical
Design of α7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies.
Universite Orleans
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
Meiji Seika Kaisha
(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity.
Sandoz Pharma
Absolute Configuration and Pharmacology of the Poison Frog Alkaloid Phantasmidine.
Indiana State University
Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.
Amgen
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.
Amgen
Discovery of β-Arrestin Biased Ligands of 5-HT
Korea Institute of Science and Technology
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.
University of The Philippines
Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor.
Bristol-Myers Squibb Pharmaceutical Research Institute
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Development of spiroguanidine-derivedα7 neuronal nicotinic receptor partial agonists.
Bristol-Myers Squibb Research and Development
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.
Virginia Commonwealth University
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Urea and amide derivatives of aminoalkylpiperazines and use thereof
Southern Research Institute
N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders
Ogeda
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.
Panjab University
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme
17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
Universitaet Des Saarlandes
BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.
Smithkline Beecham Pharmaceuticals
Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin.
Massachusetts Institute of Technology
Site-activated chelators targeting acetylcholinesterase and monoamine oxidase for Alzheimer's therapy.
The Weizmann Institute of Science
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.
University of Cambridge
Thermodynamics of molecular recognition by cyclodextrins. 1. Calorimetric titration of inclusion complexation of naphthalenesulfonates with .alpha.-, .beta.-, and .gamma.-cyclodextrins: enthalpy-entropy compensation
Himeji Institute of Technology
Chiral Recognition Thermodynamics of β-Cyclodextrin: The Thermodynamic Origin of Enantioselectivity and the Enthalpy-Entropy Compensation Effect
Japan Science and Technology Agency
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.
Dainippon Sumitomo Pharma
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Wyeth Research
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.
University of Alabama At Birmingham
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
Johnson & Johnson Pharmaceutical
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
Kinetic, thermodynamic and X-ray structural insights into the interaction of melatonin and analogues with quinone reductase 2.
University of Illinois At Chicago
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
Chalcones: a valid scaffold for monoamine oxidases inhibitors.
Sapienza University of Rome
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Wyeth Research
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Absolute Science
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
Methylgene
Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Boehringer Ingelheim (Canada)
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Tanabe Research Laboratories Usa
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Astex
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Valeant Pharmaceuticals Research and Development
Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors.
University of Southern California
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Sunesis Pharmaceuticals
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
Astrazeneca
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
Astrazeneca