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152 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28591512 114 Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.EBI Glaxosmithkline
28337332 41 BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.EBI Bristol-Myers Squibb
28169167 137 Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
2157007 9 Synthesis and alpha 2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogues in human platelets.EBI Ohio State University
7120280 9 Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety.EBI TBA
27958732 93 Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.EBI Bristol-Myers Squibb
27876250 60 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
27939174 84 Challenges in the development of an MEBI Vanderbilt University Medical Center
28105289 51 Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists.EBI Bristol-Myers Squibb Research and Development
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27933810 166 Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HTEBI National Institute of Diabetes and Digestive and Kidney Diseases
26876931 36 Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.EBI Abbott Healthcare Products
26988801 55 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
26700945 68 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
26475518 19 Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI City University of New York
25127461 36 Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.EBI Yonsei University
24901260 12 Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors.EBI University of Illinois At Chicago
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI Glaxosmithkline
24755431 59 The discovery of diazepinone-based 5-HT3 receptor partial agonists.EBI Amri
24050653 59 Derivatives of dibenzothiophene for positron emission tomography imaging ofa7-nicotinic acetylcholine receptors.EBI The Johns Hopkins University School of Medicine
24582985 1 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): a novel non-nitrogenous ligand for 5-HT2B receptor.EBI Virginia Commonwealth University
24365159 35 The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.EBI University of Missouri
24128816 10 Design of fluorinated 5-HT(4)R antagonists: influence of the basicity and lipophilicity toward the 5-HT(4)R binding affinities.EBI University of Southampton
24128813 8 Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.EBI Universit£
24147864 6 Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).EBI National Institute of Mental Health
24084296 9 In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model.EBI University of Mississippi
24035337 10 2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.EBI Virginia Commonwealth University
24611085 101 Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.EBI Sanford-Burnham Medical Research Institute
23756062 25 Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.EBI Theravance
23707254 7 Selectivity of phenothiazine cholinesterase inhibitors for neurotransmitter systems.EBI Dalhousie University
23602445 23 An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.EBI Ucl School of Pharmacy
23582449 20 Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.EBI Institute of Organic Synthesis
23466604 36 Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.EBI Universit£
23403082 28 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.EBI Broad Institute of Mit and Harvard
23414838 33 Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
23265874 1 Near native binding of a fluorescent serotonin conjugate to serotonin type 3 receptors.EBI Washington State University
22468936 49 Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789).EBI Siena Biotech
21782429 18 Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H4 and the ion channel serotonin 5-HT3A.EBI Vu University Amsterdam
20724042 2 Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.EBI University of Modena and Reggio Emilia
20591663 23 Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in silico screening methods.EBI Glaxosmithkline
9191957 210 Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.EBI Universit£
7752204 98 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
23084435 17 Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.EBI Savannah State University
21486038 177 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
23126648 213 Discovery of (2S,3R)-N-[2-(Pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selectivea7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.EBI Targacept
23102207 122 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£
23083093 25 N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): a medicinal chemistry effort toward ana7 nicotinic acetylcholine receptor agonist preclinical candidate.EBI Siena Biotech
23006002 35 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
22793665 190 Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selectivea4ß2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.EBI Targacept
23006041 32 Design, synthesis, and structure-activity relationships of highly potent 5-HT3 receptor ligands.EBI Vu University Amsterdam
21919481 114 Discovery and development ofa7 nicotinic acetylcholine receptor modulators.EBI Targacept
22313227 78 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
21726069 98 Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.EBI University of Namur
21207959 69 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
20931963 112 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.EBI Aska Pharmaceutical
20684563 176 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
20146481 16 Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.EBI University of Warwick
19963380 38 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
19700325 46 mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).EBI Sepracor
19576766 86 Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.EBI Pfizer
19447040 31 Quinazolindione derivatives as potent 5-HT3A receptor antagonists.EBI Konkuk University
18468904 48 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
18033297 3 An antidepressant that extends lifespan in adult Caenorhabditis elegans.EBI Howard Hughes Medical Institute
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18023344 77 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.EBI F. Hoffmann-La Roche
17998160 101 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI F. Hoffmann-La Roche
18181565 71 Multi-target-directed ligands to combat neurodegenerative diseases.EBI University of Bologna
17722904 146 Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.EBI University of Copenhagen
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes For Biomedical Research
16165358 26 High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.EBI Eli Lilly
12540230 18 5-HT4 receptor ligands: applications and new prospects.EBI Paris-Sud University
12954071 109 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
12825922 207 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).EBI Virginia Commonwealth University
11170628 37 Synthesis and structure-activity relationships of a new model of arylpiperazines. 5. Study of the physicochemical influence of the pharmacophore on 5-HT(1a)/alpha(1)-adrenergic receptor affinity: synthesis of a new derivative with mixed 5-HT(1a)/d(2) antagonist properties.EBI Universidad Complutense
9083484 84 New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI Cooperation Pharmaceutique Fran�Aise
2145434 11 An initial three-component pharmacophore for specific serotonin-3 receptor ligands.EBI Pfizer
2213824 20 Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.EBI Pfizer
22107017 47 Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H3 receptor antagonists with potent cognition enhancing activity.EBI Cephalon
22189135 15 High-affinity fluorescent ligands for the 5-HT(3) receptor.EBI University of Bern
21866910 66 N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT6R) antagonists with unique structural features.EBI Abbott Healthcare Products
21195614 56 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
21146988 26 Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.EBI Amri
20889341 59 Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.EBI Amri
20812727 157 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
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20709559 16 Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.EBI Purdue University
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università
20465311 36 Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).EBI Siena Biotech
20384344 42 Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI Meiji Seika Kaisha
20043678 92 Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.EBI Pfizer
19646882 72 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
19646865 45 Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.EBI Pfizer
9182127 9 Perhydrogenation of tabersonine, ans Aspidiosperma indole alkaloid.EBI UniversitÉ
 21 Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamidesEBI TBA
 44 5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI TBA
19329329 183 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
19282174 85 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.EBI Pfizer
19261477 43 Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.EBI Université
19231180 81 Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.EBI Roche Palo Alto
19208472 52 Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.EBI Novartis Institutes For Biomedical Research
19119012 20 New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.EBI Washington University
17067154 27 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.EBI Uppsala University
16971122 4 Inhibitors of unactivated p38 MAP kinase.EBI Johnson and Johnson Pharmaceutical Research and Development
16821801 35 Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship.EBI Pfizer
16361098 70 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
16055331 45 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.EBI Carlsson Research
15267230 50 Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.EBI Uppsala University
12482441 45 Development of a presynaptic 5-HT1A antagonist.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12361399 17 Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.EBI Universita Di Camerino
11784148 81 Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI Pharmazeutisches Institut Der UniversitäT Freiburg
11514154 9 5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.EBI The University of Louisiana At Monroe
10715164 57 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.EBI Virginia Commonwealth University
10543880 63 Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.EBI Universita' Degli Studi Di Salerno
10464021 59 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
9357515 55 Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.EBI Merck Sharp and Dohme Research Laboratories
8831767 60 Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.EBI Virginia Commonwealth University
1652026 43 Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.EBI Virginia Commonwealth University
24108128 2 Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis.BDB University of Wuerzburg
26833890 18 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
27064299 8 Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.BDB Broad Institute
26851737 36 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
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig
19351152 34 Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases.BDB University of Leeds
17154490 10 Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.BDB Karo Bio
16686531 26 Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.BDB Mgi Pharma
12941317 25 Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.BDB Glaxosmithkline
10698450 21 Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.BDB Medivir
 4 Molecular Origins of the Slow Streptavidin-Biotin Dissociation KineticsBDB University of Washington