394 articles for thisTarget
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Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
The University of Newcastle
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.
Pfizer
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.
Meiji Seika Kaisha
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.
Glaxosmithkline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Glaxosmithkline
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Glaxosmithkline
New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT
University of Catania
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
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.
Eli Lilly
5-HT7 receptor modulators: Amino groups attached to biphenyl scaffold determine functional activity.
Yonsei University
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.
Florida A&M University
Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.
University of Bari Aldo Moro
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Florida A&M University
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.
Jagiellonian University Medical College
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University of Illinois At Chicago
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
Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.
Jagiellonian University Medical College
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile.
Jagiellonian University Medical College
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.
Huazhong University of Science and Technology
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent.
Jagiellonian University Medical College
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.
City University of New York
Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity.
Jagiellonian University Medical College
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
University of Illinois At Chicago
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
Jagiellonian University Collegium Medicum
Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.
Jagiellonian University Medical College
Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands.
Jagiellonian University
Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands.
University of Catania
Structure-activity relationships and molecular modeling studies of novel arylpiperazinylalkyl 2-benzoxazolones and 2-benzothiazolones as 5-HT(7) and 5-HT(1A) receptor ligands.
University of Catania
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
Yonsei University
The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
Universidad Complutense De Madrid
Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2.
Astellas Pharma
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT1A receptor functional profile.
Jagiellonian University Medical College
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.
Adamed
Towards the development of 5-HT7 ligands combining serotonin-like and arylpiperazine moieties.
University of Urbino
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects.
Therachem Research Medilab (India)
SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.
Jagiellonian University Medical College
Solid-supported synthesis, molecular modeling, and biological activity of long-chain arylpiperazine derivatives with cyclic amino acid amide fragments as 5-HT(7) and 5-HT(1A) receptor ligands.
Jagiellonian University Medical College
Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT(7) ligands and role of the aromatic substituents in binding to the target receptor.
Institute of Science and Technology
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.
Glaxosmithkline
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors.
Jagiellonian University Medical College
Quantitative structure-activity relationship study of serotonin (5-HT7) receptor inhibitors using modified ant colony algorithm and adaptive neuro-fuzzy interference system (ANFIS).
Sharif University of Technology
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Glaxosmithkline
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
F. Hoffmann-La Roche
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.
Janssen-Cilag
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Organon Research and Development Group
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Smithkline Beecham Pharmaceuticals
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).
The University of Sydney
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
H. Lundbeck
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
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
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.
University of Li£Ge
Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
University of Bari Aldo Moro
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
National Institute of Biological Sciences
The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists.
TBA
Microwave assisted synthesis of spirocyclic pyrrolidines -s1 receptor ligands with modified benzene-N-distance.
Institut F£R Pharmazeutische Und Medizinische Chemie
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Florida A&M University
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
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Pfizer
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.
Universidad Complutense De Madrid
Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands.
Jagiellonian University Medical College
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S of Maine
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
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.
Egis Pharmaceuticals
Novel quinazolinone derivatives as 5-HT7 receptor ligands.
Institute of Science and Technology
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
7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands.
Jagiellonian University Medical College
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Wyeth Research
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
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).
Purdue University
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
Eli Lilly
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.
Astra Arcus
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.
Jagiellonian University Medical College
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
Florida A&M University
New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.
Universidad Complutense De Madrid
Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands.
Jagiellonian University Medical College
Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor.
Vu University Medical Center
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features.
Abbott Healthcare Products
Optimization of (arylpiperazinylbutyl)oxindoles exhibiting selective 5-HT7 receptor antagonist activity.
Egis Pharmaceuticals
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.
University of South Florida
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.
Green Cross
Synthesis and structural investigation of some pyrimido[5,4-c]quinolin-4(3H)-one derivatives with a long-chain arylpiperazine moiety as potent 5-HT(1A/2A) and 5-HT(7) receptor ligands.
Medical University of Lodz
Synthesis and biological evaluation of potential 5-HT(7) receptor PET radiotracers.
University of Lyon
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.
TBA
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor.
Vu University Medical Center
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.
Wyeth Research
Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT(7) antagonists.
Johnson & Johnson Pharmaceutical Research and Development
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.
Korea Research Institute of Chemical Technology
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Bristol-Myers Squibb
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.
Wyeth Research
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
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Purdue University
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.
Korea Research Institute of Chemical Technology
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists.
Polish Academy of Sciences
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Yangji Chemicals
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.
Green Cross
Molecular modeling study of 4-phenylpiperazine and 4-phenyl-1,2,3,6-tetrahydropyridine derivatives: a new step towards the design of high-affinity 5-HT1A ligands.
University of Li£Ge
SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling.
Orleans University
Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists.
Ewha Womans University
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
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Wyeth Research
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.
Novartis Institutes For Biomedical Research
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
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
Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.
Universidad Complutense De Madrid
Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III.
Università
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.
Korea Research Institute of Chemical Technology
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.
Wyeth Research
Preparation of piperazine derivatives as 5-HT7 receptor antagonists.
Ewha Womans University
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Uppsala University
Serotonergic activity-guided phytochemical investigation of the roots of Angelica sinensis.
University of Illinois At Chicago
Inhibition of [3H]-LSD binding to 5-HT7 receptors by flavonoids from Scutellaria lateriflora.
Tom'S of Maine
Hydrophobicity modulation via the substituents at positions 2 and 4 of 1,3,5-triazine to enhance therapeutic ability against Alzheimer's disease for potent serotonin 5-HT6R agents.
Jagiellonian University
Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for new class of drugs against Alzheimer's disease.
Jagiellonian University
5-HT6 receptor neutral antagonists protect astrocytes: A lesson from 2-phenylpyrrole derivatives.
Jagiellonian University Medical College
Design, synthesis, and biological evaluation of aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Shanghai Institute of Pharmaceutical Industry Co., Ltd.
Halogen Bonding Hot Spots as a Constraint in Virtual Screening: A Case Study of 5-HT7R.
Polish Academy of Sciences
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Korea Research Institute of Chemical Technology
Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT2 Receptor Agonist.
Cybin IRL
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
National Institute of Diabetes and Digestive and Kidney Disease
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
Glaxosmithkline
Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.
Università
M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds.
University of Strathclyde
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
Jagiellonian University Medical College
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
High Point University
Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT
University of Sassari
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
New N-aryl-N'-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT
Cracow University of Technology
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Alcon Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
F. Hoffmann-La Roche
Design, synthesis, and behavioral evaluation of dual-acting compounds as phosphodiesterase type 10A (PDE10A) inhibitors and serotonin ligands targeting neuropsychiatric symptoms in dementia.
Jagiellonian University Medical College
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
Abbott
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
Columbia University College of Physicians and Surgeons
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Carlsson Research
Phenylpyrroles, a new chemolibrary virtual screening class of 5-HT7 receptor ligands.
Université
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Janssen-Cilag
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
Johnson & Johnson Pharmaceutical Research & Development
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
Beijing Normal University
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
Uppsala University
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Wyeth Research
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.
Università
The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.
Polish Academy of Sciences
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
State University of Groningen
Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.
Jagiellonian University Medical College
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Merck
Discovery of G Protein-Biased Ligands against 5-HT
Korea Institute of Science and Technology
Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
Uppsala University
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.
Merck Sharp & Dohme Research Laboratories
Discovery of G Protein-Biased Antagonists against 5-HT
Korea Institute of Science and Technology
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Cracow University of Technology
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.
Florida A&M University
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.
Eli Lilly
Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT
Jagiellonian University Medical College
Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
University of Perugia
Privileged scaffold-based design to identify a novel drug-like 5-HT
University of Bari Aldo Moro
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
Normandie Univ
Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.
Universidad Complutense
Identification of a novel series of selective 5-HT7 receptor antagonists.
Glaxosmithkline
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
Università
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
Westf£Lische Wilhelms-Universit£T M£Nster
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT(7) receptor ligands.
Nps Pharmaceuticals
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.
Yale University
A study of the structure-affinity relationship in SYA16263; is a D
Florida A&M University
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
Jagiellonian University Medical College
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT
Janssen Research & Development
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
Merck Sharp & Dohme Research Laboratories
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.
Polish Academy of Sciences
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.
Cracow University of Technology
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
Glaxosmithkline
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT
City University of New York
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.
Columbia University College of Physicians and Surgeons
Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists.
Uppsala University
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.
Uppsala University
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.
Virginia Commonwealth University
South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.
National Institute of Diabetes and Digestive and Kidney Diseases
Design and synthesis of new homo and hetero bis-piperazinyl-1-propanone derivatives as 5-HT7R selective ligands over 5-HT1AR.
University of Catania
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.
Jagiellonian University Medical College
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (σ
Memorial Sloan Kettering Cancer Center
Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
Uppsala University
2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.
Virginia Commonwealth University
Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT
China Pharmaceutical University
Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT
China State Institute of Pharmaceutical Industry
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
Merck Sharp & Dohme Research Laboratories
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
Medical University of Warsaw
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
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT
Polish Academy of Sciences
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina at Chapel Hill
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.
Cracow University of Technology
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.
Agouron Pharmaceuticals
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT
Medical University of Warsaw
Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT
Jagiellonian University
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
Northwest University
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
Jagiellonian University Medical College
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Medical University of Warsaw
[1]Benzothieno[3,2-d]pyrimidine derivatives as ligands for the serotonergic 5-HT
University of Catania
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.
Cracow University of Technology
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.
Astellas Pharma
New 1-arylindoles based serotonin 5-HT7 antagonists. Synthesis and binding evaluation studies.
University of Lyon
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.
University of Bari Aldo Moro
Synthesis and evaluation of 1-[2-(4-[(11)C]methoxyphenyl)phenyl]piperazine for imaging of the serotonin 5-HT7 receptor in the rat brain.
National Institute of Radiological Sciences
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Jagiellonian University Medical College
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
Glaxosmithkline
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Solvay Pharma
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.
Merck Sharp and Dohme Research Laboratories
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Glaxosmithkline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Glaxosmithkline
Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives.
Universidad Complutense
Characterization of the 5-HT(7) receptor. Determination of the pharmacophore for 5-HT(7) receptor agonism and CoMFA-based modeling of the agonist binding site.
State University of Groningen
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.
Glaxosmithkline R&D
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
Meiji Seika Kaisha
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Huazhong University of Science and Technology
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT
Shanghai Institute of Pharmaceutical Industry
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Jagiellonian University Medical College
Amino Acid Hot Spots of Halogen Bonding: A Combined Theoretical and Experimental Case Study of the 5-HT
Polish Academy of Sciences
Discovery of β-Arrestin Biased Ligands of 5-HT
Korea Institute of Science and Technology
Structure-Activity Relationships and Therapeutic Potentials of 5-HT
University of Catania
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.
Jagiellonian University Medical College
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.
University of The Philippines
MF-8, a novel promising arylpiperazine-hydantoin based 5-HT
Jagiellonian University Medical College
Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT
Shanghai Institute of Pharmaceutical Industry
Structural insights into serotonin receptor ligands polypharmacology.
Polish Academy of Sciences
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT
Jagiellonian University Medical College
Novel naphthyloxy derivatives - Potent histamine H
Jagiellonian University Medical College
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
Jagiellonian University Medical College
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
EPOXYAMIDES AS KRAS G12C AND KRAS G12D INHIBITORS AND METHODS OF USING THE SAME
Amgen
Phenyl-3,4-dihydroisoquinolin-2(1h)-yl-ethan-1-one derivatives as dopamine d1receptor positive allosteric modulators
Eli Lilly
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
H. Lundbeck
Pyrrole heteroaryl ring derivative and method of use thereof
Jiangsu Hengrui Medicine
C5-C6-carbocyclic fused iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
TBA
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
Inhibitors of PTP4A3 for the treatment of cancer
University of Virginia Patent Foundation
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
Substituted dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-ones as RIPK3 inhibitors
Bristol-Myers Squibb
Substituted nicotinimide inhibitors of BTK and their preparation and use in the treatment of cancer, inflammation and autoimmune disease
Guangzhou Innocare Pharma Tech
Imaging histone deacetylases with a radiotracer using positron emission tomography
The General Hospital
Pharmaceutical compositions and methods of use of 4-pregenen-11β-17-21-triol-3,20-dione derivatives
Allergan
Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof
Taiho Pharmaceutical
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles
Hacettepe University
Pseudodipeptides as MMP inhibitors
French Alternative Energies and Atomic Energy Commission
Inhibition of apurinic/apyrimidinic endonuclease I's redox activity revisited.
Indiana University School of Medicine
Triazolo and tetrazolo pyrimidine derivatives as HNE inhibitors for treating COPD
Bayer Intellectual Property
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.
National Cancer Institute-Frederick
Adenosine receptor agonists: synthesis and biological evaluation of the diastereoisomers of 2-(3-hydroxy-3-phenyl-1-propyn-1-yl)NECA.
UniversitÀ
Prostacyclin receptors of a neuronal hybrid cell line. Divalent citations and ligand-receptor coupling.
Royal Postgraduate Medical School
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
Impact of linker strain and flexibility in the design of a fragment-based inhibitor.
Johns Hopkins University
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 the molecular and chiral recognition of cycloalkanols and camphor by modified beta-cyclodextrins possessing simple aromatic tethers.
Nankai University
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
Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.
Cnr
Identification of inhibitors of checkpoint kinase 1 through template screening.
The Institute of Cancer Research
Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.
Purdue University
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Yale University
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
Yale University
Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.
Banyu Pharmaceutical
2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists.
Banyu Pharmaceutical
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
Harvard Medical School
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale
Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.
Universita Di Siena
Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.
Tanabe Research Laboratories Usa
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Bristol-Myers Squibb
CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo.
Celera Genomics
Synthesis of novel beta-lactone inhibitors of fatty acid synthase.
The Burnham Institute For Medical Research