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430 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.EBI
University of Illinois at Chicago
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HTEBI
Bristol-Myers Squibb Co.
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Synthesis and alpha 2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogues in human platelets.EBI
Ohio State University
Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety.EBI
TBA
Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics.EBI
Universidad de Santiago de Compostela
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.EBI
Meiji Seika Kaisha, Ltd
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.EBI
GlaxoSmithKline
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.EBI
GlaxoSmithKline
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.EBI
GlaxoSmithKline
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.EBI
GlaxoSmithKline
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?EBI
UCB Pharma SA
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.EBI
SmithKline Beecham Pharmaceuticals Ltd
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.EBI
SmithKline Beecham Pharmaceuticals Ltd
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI
Jagiellonian University Medical College
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.EBI
Eli Lilly and Company
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HTEBI
Arena Pharmaceuticals
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University of Kansas
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HTEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI
Florida A&M University
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.EBI
Florida A&M University
New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.EBI
City University of New York
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.EBI
Shanghai Institute of Materia Medica
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.EBI
Abbott Healthcare Products BV
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI
Jagiellonian University Medical College
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.EBI
University of Illinois at Chicago
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.EBI
National Institute of Biological Sciences, Beijing
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists.EBI
Yonsei University
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.EBI
Universit£ de Lille
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.EBI
Gedeon Richter Plc
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI
The Alexander Shulgin Research Institute
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.EBI
University of Copenhagen
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI
City University of New York
High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice.EBI
National Institute on Drug Abuse-Intramural Research Program
Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists.EBI
University of Copenhagen
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.EBI
City University of New York
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.EBI
University of Cambridge
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.EBI
University of Illinois at Chicago
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI
Jagiellonian University Collegium Medicum
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
Novel 4-substituted-N,N-dimethyltetrahydronaphthalen-2-amines: synthesis, affinity, and in silico docking studies at serotonin 5-HT2-type and histamine H1 G protein-coupled receptors.EBI
University of Florida
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.EBI
Ewha Womans University
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.EBI
Yonsei University
Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2.EBI
Astellas Pharma Inc
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
GlaxoSmithKline
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.EBI
Universit£ degli Studi di Siena
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands.EBI
University of Copenhagen
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors.EBI
Pfizer Inc
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI
Adamed Ltd.
Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists.EBI
Cephalon Inc
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects.EBI
Therachem Research Medilab (India) Pvt. Ltd.
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.EBI
Intra-Cellular Therapies Inc
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.EBI
GlaxoSmithKline
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.EBI
Bristol-Myers Squibb Co.
[11C]olanzapine, radiosynthesis and lipophilicity of a new potential PET 5-HT2 and D2 receptor radioligand.EBI
Indiana University School of Medicine
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.EBI
Universidade Federal de Goi£s
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.EBI
University of Copenhagen
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.EBI
Bristol-Myers Squibb Research and Development
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI
Janssen-Cilag S.A.
 
Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine.EBI
TBA
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.EBI
GlaxoSmithKline
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.EBI
Universidad de Santiago de Compostela
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.EBI
GlaxoSmithKline
Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.EBI
Universidad de Santiago de Compostela
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.EBI
GlaxoSmithKline
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.EBI
GlaxoSmithKline
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.EBI
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.EBI
F. Hoffmann-La Roche Inc
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.EBI
Universit£ de Caen
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.EBI
Universit£ de Caen
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.EBI
Merck Sharp & Dohme Research Laboratories
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.EBI
Merck Sharp and Dohme Research Laboratories
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 2.EBI
Janssen-Cilag S.A.
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.EBI
Janssen-Cilag S.A.
First tricyclic oximino derivatives as 5-HT3 ligands.EBI
Universit£ de Caen
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).EBI
SmithKline Beecham Pharmaceuticals Ltd
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).EBI
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.EBI
H. Lundbeck A/S
From a4▀2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.EBI
TBA
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.EBI
Universit£ de Caen Basse-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.EBI
Suven Life Sciences Ltd
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.EBI
TBA
Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists.EBI
University of North Carolina at Chapel Hill
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI
National Institute of Biological Sciences
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.EBI
Florida A&M University
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI
Amgen Inc
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.EBI
National Institute of Mental Health
Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines.EBI
Takeda Pharmaceutical Co., Ltd
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.EBI
TBA
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists.EBI
Monash University (Parkville Campus)
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI
National Institute of Mental Health
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.EBI
H. Lundbeck A/S
Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.EBI
University of North Texas Health Science Center
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI
Hunter College and the Graduate Center of the City University of New York
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.EBI
Universitat de Barcelona
Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.EBI
Virginia Commonwealth University
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI
Purdue University
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.EBI
EGIS Pharmaceuticals Plc
Novel quinazolinone derivatives as 5-HT7 receptor ligands.EBI
Institute of Science and Technology
Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.EBI
Astellas Pharma Inc
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.EBI
Astellas Pharma Inc
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.EBI
F. Hoffmann-La Roche Inc
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.EBI
Johnson & Johnson Pharmaceutical Research and Development LLC
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI
F. Hoffmann-La Roche Inc
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.EBI
Merck Sharp and Dohme Research Laboratories
Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.EBI
Bayer Pharmaceuticals Corporation
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.EBI
Organix Inc
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.EBI
Pfizer Inc
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes for BioMedical Research
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.EBI
Universit£ degli Studi di Urbino Carlo Bo
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.EBI
Wyeth Research
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750.EBI
Pfizer Inc
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical Inc.
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.EBI
H. Lundbeck A/S
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.EBI
Alcon Research Ltd
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).EBI
Virginia Commonwealth University
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
Current and novel approaches to the drug treatment of schizophrenia.EBI
Merck Sharp and Dohme Research Laboratories
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.EBI
Eli Lilly and Company
From hit to lead. Analyzing structure-profile relationships.EBI
Universities of Lille
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI
Cooperation Pharmaceutique Fran�aise
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.EBI
Abbott Laboratories
Central serotonin receptors as targets for drug research.EBI
TBA
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI
Virginia Commonwealth University
Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.EBI
Arena Pharmaceuticals Inc
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.EBI
Cephalon Inc
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.EBI
Florida A&M University
Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).EBI
University of Lille
5-HT2c receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs.EBI
Korea Institute of Science and Technology
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features.EBI
Abbott Healthcare Products BV
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI
University of South Florida
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.EBI
Green Cross Corporation
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.EBI
University of Copenhagen
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.EBI
Pfizer Inc
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.EBI
Wyeth Research
Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders.EBI
Evotec UK Ltd
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.EBI
Korea Research Institute of Chemical Technology
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.EBI
Bristol-Myers Squibb Co.
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.EBI
Wyeth Research
Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI
Green Cross Corporation
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.EBI
University of Copenhagen
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI
National Institute of Mental Health
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical and Public Health Institute
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.EBI
CSIRO Molecular and Health Technologies
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.EBI
Korea Research Institute of Chemical Technology
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.EBI
Arena Pharmaceuticals
Further optimization of novel pyrrole 3-carboxamides for targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI
Green Cross Corporation
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.EBI
Merck Sharp & Dohme
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.EBI
Arena Pharmaceuticals
8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.EBI
Chemical Diversity Research Institute
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.EBI
Yangji Chemicals
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.EBI
Pfizer Inc
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI
Green Cross Corporation
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.EBI
Amgen Inc
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.EBI
Bristol-Myers Squibb Co.
Synthesis and biological evaluation of (phenylpiperazinyl-propyl)arylsulfonamides as selective 5-HT(2A) receptor antagonists.EBI
Ewha Womans University
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.EBI
Pfizer Inc
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and the Informatics Institute of UMDNJ
Design and synthesis of pyridazinone-based 5-HT(2C) agonists.EBI
Pfizer Inc
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists.EBI
Pfizer Inc
Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agents.EBI
Arena Pharmaceuticals Inc
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.EBI
Pfizer Inc
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.EBI
Wyeth Research
Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.EBI
Universitat de Barcelona
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.EBI
Novartis Institutes for BioMedical Research
Identification of novel serotonin 2C receptor ligands by sequential virtual screening.EBI
Institute of Science and Technology
 
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonistsEBI
TBA
 
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamidesEBI
TBA
 
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI
TBA
 
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI
TBA
 
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.EBI
TBA
 
Novel conformationally restricted aromatic piperidines as selective sigma receptor ligandsEBI
TBA
 
Novel ether derivatives of alkyl piperidines as potential sigma / 5HT2 antipsychotic agentsEBI
TBA
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.EBI
University of Illinois at Chicago
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.EBI
Pfizer Inc
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.EBI
Florida A&M University
Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.EBI
National Institute on Drug Abuses
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.EBI
Pfizer Inc
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.EBI
Korea Research Institute of Chemical Technology
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.EBI
Florida A&M University
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands.EBI
Wyeth Research
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.EBI
GlaxoSmithKline
Preparation of piperazine derivatives as 5-HT7 receptor antagonists.EBI
Ewha Womans University
Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.EBI
Uppsala University
New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea.EBI
The University of Mississippi
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.EBI
Korea Research Institute of Chemical Technology
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.EBI
National Institute on Drug Abuse-Intramural Research Program
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.EBI
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
GlaxoSmithKline
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.EBI
Cerep
Novel sigma receptor ligands: synthesis and biological profile.EBI
University of Catania
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.EBI
Pharmaceutical Research Institute
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.EBI
Procter and Gamble Pharmaceuticals
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.EBI
Procter & Gamble Pharmaceuticals
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.EBI
Merck Sharp and Dohme Research Laboratories
Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.EBI
Procter and Gamble Pharmaceuticals Inc
The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.EBI
Athersys Inc
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI
Pfizer Inc
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.EBI
Predix Pharmaceuticals Ltd.
A new class of selective, non-basic 5-HT2A receptor antagonists.EBI
Merck Sharp & Dohme
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.EBI
Florida A&M University
The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists.EBI
Athersys Inc
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.EBI
Alcon Research Ltd
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.EBI
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.EBI
F. Hoffmann-La Roche Inc
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.EBI
Vernalis plc
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.EBI
Abbott GmbH & Co. KG
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI
Columbia University College of Physicians and Surgeons
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.EBI
7TM Pharma A/S
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.EBI
Organix Inc
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.EBI
Carlsson Research AB
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.EBI
Merck Sharp and Dohme Research Laboratories
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.EBI
Vernalis Research Ltd
Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism.EBI
Janssen-Cilag S.A.
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI
Janssen-Cilag S.A.
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI
Johnson & Johnson Pharmaceutical Research & Development
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.EBI
Arena Pharmaceuticals Inc
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.EBI
Wyeth Research
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Aminotriazine 5-HT7 antagonists.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.EBI
Argenta Discovery Limited
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.EBI
Pfizer Inc
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HTEBI
Jagiellonian University Medical College
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists.EBI
Janssen-Cilag S.A.
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.EBI
Wyeth Research
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DEBI
ShanghaiTech University
Synthesis and biological evaluation of 1-(4-(piperazin-1-yl)phenyl)pyridin-2(1H)-one derivatives as potential SSRIs.EBI
Sunshine Lake Pharma Co. Ltd.
Indoline derivatives as 5-HT(2C) receptor agonists.EBI
Vernalis Research Ltd
Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).EBI
Virginia Commonwealth University
Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HTEBI
Sunshine Lake Pharma Co. Ltd.
Discovery of G Protein-Biased Antagonists against 5-HTEBI
Korea Institute of Science and Technology
Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI
Virginia Commonwealth University
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.EBI
Cracow University of Technology
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.EBI
Neurogen Corporation
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.EBI
Huazhong University of Science and Technology
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.EBI
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.EBI
Eli Lilly and Company
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.EBI
Pharmacia Corporation
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.EBI
University of Sydney
Identification of a novel series of selective 5-HT7 receptor antagonists.EBI
GlaxoSmithKline
Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.EBI
Bristol-Myers Squibb Co.
Synthesis and SAR Studies of 1EBI
University of Nebraska Medical Center
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.EBI
Jiangsu Ocean University
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.EBI
Université de Caen
Development of a presynaptic 5-HT1A antagonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.EBI
University of Florida
Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT4R) partial agonist and 5-HT6R antagonist activities, as potential treatment of Alzheimer's disease.EBI
Normandie Universit£
Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives.EBI
EGIS Pharmaceuticals Ltd.
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.EBI
Universita di Camerino
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HTEBI
Arena Pharmaceuticals
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.EBI
Westf£lische Wilhelms-Universit£t M£nster
Isoquinolinone derivatives as potent CNS multi-receptor DEBI
Jiangsu Ocean University
Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior.EBI
University of Texas Medical Branch
Structure activity relationship of novel antiviral nucleosides against Enterovirus A71.EBI
National Institute of Diabetes and Digestive and Kidney Disease
Synthesis, receptor potency, and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging.EBI
Yale University
A study of the structure-affinity relationship in SYA16263; is a DEBI
Florida A&M University
The Essential Medicinal Chemistry of Cannabidiol (CBD).EBI
University of Minnesota
Design and Discovery of Functionally Selective Serotonin 2C (5-HTEBI
University of Illinois at Chicago
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HTEBI
Janssen Research & Development, LLC
Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.EBI
Virginia Commonwealth University
Structure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HTEBI
Kalamazoo College
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.EBI
GlaxoSmithKline
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTREBI
Dominican College
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI
Columbia University College of Physicians and Surgeons
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.EBI
University of Chinese Academy of Sciences
Discovery of a lead series of potent benzodiazepine 5-HTEBI
Arena Pharmaceuticals
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge EBI
University of Mississippi
Evaluation of anti-depressant effects of phthalazinone-based triple-acting small molecules against 5-HTEBI
Korea Institute of Science and Technology
2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.EBI
Merck Sharp & Dohme Research Laboratories
Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.EBI
Wyeth-Ayerst Research
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.EBI
National Institute on Drug Abuse-Intramural Research Program
Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.EBI
NPS Allelix Corp.
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity.EBI
Yoshitomi Pharmaceutical Industries Ltd
Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines.EBI
Pfizer Inc.
Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HTEBI
CSIR-Central Drug Research Institute (CSIR-CDRI)
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.EBI
SmithKline Beecham Pharmaceuticals Ltd
Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine DEBI
National Institute on Drug Abuse-Intramural Research Program
Identification of a novel DGK? inhibitor for XLP-1 therapy by virtualáscreening.EBI
University of Piemonte Orientale
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.EBI
ShanghaiTech University
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.EBI
Knoll Pharmaceuticals
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI
University of Pennsylvania
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.EBI
National University of Ireland Galway
Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine.EBI
Purdue University
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HTEBI
Harvard Medical School
Design and in Vivo Characterization of AEBI
Medical College of Wisconsin
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HTEBI
University of Illinois at Chicago
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.EBI
Purdue University
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives.EBI
Purdue University
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.EBI
Northwest University
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity.EBI
Purdue University
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.EBI
Institut de Chimie Pharmaceutique Albert Lespagnol
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.EBI
Merck Sharp and Dohme Research Laboratories
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives.EBI
Purdue University
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.EBI
Università di Catania
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.EBI
Medical University of Warsaw
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.EBI
TBA
Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HTEBI
TBA
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University of Minnesota Twin Cities
Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups.EBI
Purdue University
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI
Janssen Pharmaceutica N.V.
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.EBI
Astellas Pharma Inc
Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization.EBI
Harvard Medical School
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.EBI
Universidade Federal do Rio de Janeiro
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.EBI
Bristol-Myers Squibb Research and Development
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory AS
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.EBI
Arena Pharmaceuticals Inc.
Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics.EBI
Universidad de Santiago de Compostela
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.EBI
GlaxoSmithKline
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.EBI
Solvay Pharma
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.EBI
GlaxoSmithKline
Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation.EBI
GlaxoSmithKline Medicine Research Centre
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.EBI
GlaxoSmithKline
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI
GlaxoSmithKline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.EBI
GlaxoSmithKline
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp.EBI
GlaxoSmithKline R&D
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.EBI
Meiji Seika Kaisha Ltd.
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.EBI
GlaxoWellcome
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.EBI
Universidad de Santiago
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.EBI
SmithKline Beecham Pharmaceuticals
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.EBI
F. Hoffmann-La Roche Inc
(+)-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.EBI
Sandoz Pharma Ltd.
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI
Texas Tech University Health Sciences Center
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.EBI
Shanghai Institute of Materia Medica
Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MTEBI
Univ. Lille
5-HTEBI
Usona Institute
Discovery of ?-Arrestin Biased Ligands of 5-HTEBI
Korea Institute of Science and Technology
Structure-Activity Relationships and Therapeutic Potentials of 5-HTEBI
Universit£ di Catania
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.EBI
University of the Philippines
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.EBI
University of Chinese Academy of Sciences
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
University of Texas at Austin
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.EBI
Pfizer Inc
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HEBI
GlaxoSmithKline
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide.EBI
Taisho Pharmaceutical Co., Ltd
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.EBI
Xinjiang Technical Institute of Physics and Chemistry
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI
Northwestern University
Return of DEBI
University of Nebraska Medical Center
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.EBI
St. John's University
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.EBI
Harvard Medical School
A Positive Allosteric Modulator of the Serotonin 5-HTEBI
Universidad Complutense de Madrid
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.EBI
Pfizer Inc
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.EBI
Upjohn Company
Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines.BDB
Giresun University
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB
Yogi Vemana University
The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter.BDB
Jagiellonian University Medical College
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.BDB
Broad Institute
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.BDB
University of Washington
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.BDB
Chulabhorn Research Institute
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB
Peking University
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.BDB
University of Karachi
Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast a-glucosidase, acetylcholinesterase and butyrylcholinesterase.BDB
GC University
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.BDB
Tehran University of Medical Sciences
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
Structure and Inhibition of Microbiome ▀-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.BDB
University of North Carolina at Chapel Hill
Monoamine oxidase inhibitory activity of 2-aryl-4H-chromen-4-ones.BDB
Birla Institute of Technology
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes.BDB
COMSATS Institute of Information Technology
Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.BDB
The Royal Danish School of Pharmacy
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach.BDB
University of Bonn
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.BDB
Abbott Laboratories
In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist.BDB
Whitby Research, Inc.
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.BDB
Abbott Laboratories
Neuroleptic binding to human brain receptors: relation to clinical effects.BDB
Mayo Clinic
Molecular cloning and characterization of a rat brain cDNA encoding a 5-hydroxytryptamine1B receptor.BDB
University of Heidelberg
Rhodanine derivatives as selective protease inhibitors against bacterial toxins.BDB
Burnham Institute for Medical Research