BindingDB logo
myBDB logout

422 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28244748 119 The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.EBI Virginia Commonwealth University
28017532 140 Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.EBI AstraZeneca
28435524 47 Pyrano[2,3,4-EBI Polish Academy of Sciences
8515429 16 (+/-) 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
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
12467617 17 New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability.EBI Meiji Seika Kaisha Ltd.
12392747 36 SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.EBI GlaxoSmithKline
11992776 70 Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.EBI GlaxoSmithKline
11266169 27 Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.EBI SmithKline Beecham Pharmaceuticals
11597412 116 Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.EBI GlaxoSmithKline
27689727 46 Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HTEBI Universit£ degli Studi di Modena e Reggio Emilia
28063784 36 New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HTEBI Universit£ di Catania
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
27908761 55 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
27487565 169 Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.EBI Shanghai Jiao Tong University
27865645 62 Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HTEBI Sumitomo Dainippon Pharma Co., Ltd.
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27717652 275 Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI Florida A&M University
27692547 7 Synthesis and activity of newly designed aroxyalkyl or aroxyethoxyethyl derivatives of piperazine on the cardiovascular and the central nervous systems.EBI Jagiellonian University Medical College
27318552 126 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.EBI Universit£ degli Studi di Bari"A. Moro"
27364609 230 Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.EBI Florida A&M University
27312422 219 Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.EBI Florida A&M University
27173799 97 Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.EBI Shanghai Institute of Materia Medica
26954848 38 Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.EBI Takeda Pharmaceutical Company Limited
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 B.V.
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
26900658 56 Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.EBI Jagiellonian University Medical College
26874044 56 Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.EBI Universit£ di Modena e Reggio Emilia
26704965 229 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
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
26852005 82 Novel N-acyl-carbazole derivatives as 5-HT7R antagonists.EBI Yonsei University
26698537 93 Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.EBI Jagiellonian University Medical College
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26706111 72 N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile.EBI Jagiellonian University Medical College
26271587 17 Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores.EBI Lilly Research Laboratories
26227779 37 Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.EBI Fudan University
26203768 104 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
25288493 96 Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines.EBI 25288493
25261823 107 Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors.EBI Universit£ degli Studi di Modena e Reggio Emilia
26081758 18 Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment ofß-arrestin-2.EBI Karolinska Institute and Karolinska University Hospital
25695425 62 Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.EBI City University of New York
25633969 96 Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.EBI University of Illinois at Chicago
25557493 109 Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI Jagiellonian University Collegium Medicum
25555143 60 Towards novel 5-HT7versus 5-HT1A receptor ligands among LCAPs with cyclic amino acid amide fragments: design, synthesis, and antidepressant properties. Part II.EBI Jagiellonian University Medical College
25489882 63 Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.EBI Northwestern University
25866241 88 Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands.EBI Jagiellonian University
25759032 55 Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT1A and 5-HT7 receptor ligands.EBI Universit£ di Catania
25128671 65 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.EBI Universit£ di Catania
25127461 36 Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.EBI Yonsei University
25073094 24 The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.EBI Universidad Complutense de Madrid
25070422 126 Further evaluation of the tropane analogs of haloperidol.EBI Florida A&M University
25556097 70 Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.EBI Washington University School of Medicine
25343529 221 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
25308766 56 Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.EBI Chinese Academy of Sciences
25241924 47 The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.EBI Novartis Institutes for BioMedical Research
25182564 38 Synthesis and evaluation of arylpiperazines derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands.EBI Stony Brook University
24878222 50 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.
24805037 380 Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI Adamed Ltd.
24800940 146 Identification of a new selective dopamine D4 receptor ligand.EBI Florida A&M University
24900840 35 Enhancing a CH-? Interaction to Increase the Affinity for 5-HT1A Receptors.EBI University of Li£ge
24559051 141 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.
24691057 62 SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.EBI Jagiellonian University Medical College
24675176 74 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.EBI Jagiellonian University Medical College
23252794 56 Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives ina1-adrenergic and 5-HT1A receptor binding sites recognition.EBI University of Camerino
16730983 165 Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.EBI GlaxoSmithKline Psychiatry Centre of Excellence for Drug Discovery
23477943 51 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 Company
23332346 69 Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.EBI Chinese Academy of Sciences
23425156 24 The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.EBI Novartis Pharma AG
23279866 69 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.EBI Jagiellonian University Medical College
18162395 89 Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.EBI Novartis Institutes for BioMedical Research
12443779 44 2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI Johnson& Johnson Pharmaceutical Research& Development
 18 Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine.EBI TBA
24900506 39 Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.EBI TBA
22370341 29 Favourable involvement ofa2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement.EBI University of Camerino
22145629 68 Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors.EBI Universit£ degli Studi di Modena e Reggio Emilia
17562349 66 A chemometric study of the 5-HT(1A) receptor affinities presented by arylpiperazine compounds.EBI Universidade de S£o Paulo
20951584 105 5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.EBI GlaxoSmithKline
20801662 60 Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.EBI Universit£ di Bari
20605276 61 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.EBI Universit£ degli Studi di Modena e Reggio Emilia
20133028 88 Pharmacophore-based 3D QSAR studies on a series of high affinity 5-HT1A receptor ligands.EBI Universidade Federal da Para£ba
20185311 72 Discovery of a new series of 5-HT1A receptor agonists.EBI Universit£ degli Studi di Modena e Reggio Emilia
19846239 24 Application of desirability-based multi(bi)-objective optimization in the design of selective arylpiperazine derivates for the 5-HT1A serotonin receptor.EBI University of Porto
19071020 66 Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.EBI GlaxoSmithKline
19286377 101 8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.EBI GlaxoSmithKline
18799312 84 6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.EBI GlaxoSmithKline
18817363 84 Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.EBI Universit£ di Camerino
18829312 64 Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.EBI GlaxoSmithKline
18433113 124 Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.EBI GlaxoSmithKline
16039851 57 8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands.EBI GlaxoSmithKline
9548813 53 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
9191957 210 Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.EBI Universit£ de Caen
8642566 277 Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.EBI Universit£ de Caen
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
8496922 92 Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.EBI Merck Sharp and Dohme Research Laboratories
11755365 113 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
11755364 104 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
11229746 6 First tricyclic oximino derivatives as 5-HT3 ligands.EBI Universit£ de Caen
11140733 92 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
9873561 29 Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.EBI Solvay Pharma
9871765 14 Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.EBI University of Bologna
 68 The discovery of a series of new non-indole 5HT1D agonistsEBI TBA
23043306 69 Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.EBI NeuroSearch Sweden AB
22795332 66 Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012.EBI F. Hoffmann-La Roche Ltd
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 A/S
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£ de Caen Basse-Normandie
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 Ltd.
22533875 11 Mitigating heterocycle metabolism in drug discovery.EBI Amgen, Inc
22845053 100 Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists.EBI University of North Carolina at Chapel Hill
22738628 38 Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors.EBI University of Li£ge
22738316 35 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.EBI Universit£ degli Studi di Bari A. Moro
22694093 16 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI National Institute of Biological Sciences
22926225 200 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.EBI TBA
24900202 38 Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI TBA
22748706 52 Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor.EBI Shenyang Pharmaceutical University
22520153 135 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
22607670 34 Interactions of N-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-2-aryl-2-yl-acetamides and 1-{[2-(4-phenyl-piperazin-1-yl)-ethyl]-phenyl}-3-aryl-2-yl-ureas with dopamine D2 and 5-hydroxytryptamine 5HT(1A) receptors.EBI University of Belgrade
22542010 31 Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI Amgen San Francisco
22313242 146 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI Pfizer Inc.
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
22268448 34 New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.EBI University of Li£ge
21859078 62 Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity.EBI Institut f£r Pharmazeutische und Medizinische Chemie der Universit£t M£nster
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 Co, Ltd
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 A/S
20041669 85 Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.EBI Chinese Academy of Sciences
20153652 49 Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.EBI Universidade Federal do Rio Grande do Sul
19754201 2 Physical binding pocket induction for affinity prediction.EBI University of California
19705871 14 Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure.EBI Universita degli Studi di Bari
19559623 33 'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity.EBI Chinese Academy of Sciences
19331412 122 N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.EBI National Institute on Drug AbuseIntramural Research Program
19159187 38 Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.EBI Universitat de Barcelona
18834188 232 Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2.EBI Wyeth Research
16562853 22 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.EBI Tom's of Maine
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
18083580 118 Novel quinazolinone derivatives as 5-HT7 receptor ligands.EBI Institute of Science and Technology
18221879 13 Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.EBI Westf£lische Wilhelms-Universit£t M£nster
18269229 16 N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands.EBI Universita degli Studi di Bari
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18029187 20 Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.EBI University of Missouri-Columbia
18023344 77 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.EBI F. Hoffmann-La Roche Ltd
17998160 101 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI F. Hoffmann-La Roche Ltd
18181565 71 Multi-target-directed ligands to combat neurodegenerative diseases.EBI University of Bologna
16854086 96 Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.EBI Wyeth Research
16789750 155 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.EBI Laboratoire de Chimie Th�rapeutique
16480278 279 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.EBI Organix Inc.
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes for BioMedical Research
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15801844 25 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.EBI Universidad Complutense
15658848 103 Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.EBI Wyeth Research
15916420 68 Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.EBI Friedrich Alexander University
15887953 16 Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.EBI Wyeth Research
15634021 113 Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.EBI Universit£ di Modena and Reggio Emilia
15357957 29 Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.EBI Brigham& Women's Hospital
15239663 60 Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.EBI Abbott Laboratories
12519065 243 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
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, Ltd.
12825922 207 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).EBI Virginia Commonwealth University
12361386 113 Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.EBI Friedrich-Alexander University
12213075 70 Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).EBI Purdue University
11170639 73 Current and novel approaches to the drug treatment of schizophrenia.EBI Merck Sharp and Dohme
11708905 20 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 Lilly Research Laboratories
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI F-59000 Lille
10602703 73 A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.EBI Warner-Lambert Company
9083484 84 New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI Cooperation Pharmaceutique Fran�aise
8568804 42 New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.EBI Universit£ di Bari
7562938 17 New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.EBI Wyeth-Ayerst Research
7658447 72 Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.EBI Centre de Recherche Pierre Fabre
7608898 4 The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.EBI Sandoz Pharma Limited
8097538 69 Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.EBI Upjohn Laboratories
8101876 28 Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants.EBI Upjohn Laboratories
8496900 136 Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands.EBI Upjohn Laboratories
1348089 71 Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.EBI Upjohn Laboratories
15203136 39 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
11844688 102 Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.EBI Friedrich-Alexander University
12113813 53 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.EBI Friedrich-Alexander University
11549463 72 Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).EBI Friedrich-Alexander University
10576696 32 Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.EBI Merck
 25 Pyrazolo[1,5-a]pyridines and pyrazolo[1,5-b]pyridazines as 5ht3-antagonistsEBI TBA
22336245 72 Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.EBI Florida A&M University
22309909 37 Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.EBI National Medicines Institute
22245230 128 Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI Florida A&M University
22029386 156 New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage.EBI Universidad Complutense de Madrid
22000209 54 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.EBI VU University Medical Center
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 B.V.
21782428 61 Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.EBI Lundbeck Research USA, Inc.
21907583 48 CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI University of South Florida
21899931 27 Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.EBI The University of Mississippi
21823597 373 Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.EBI Green Cross Corporation
21783363 10 Synthesis and in vitro evaluation of derivatives of theß¿?-adrenergic receptor antagonist HX-CH 44.EBI University of Toronto
21732626 60 Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.EBI Washington University
21591752 41 Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.EBI Soochow University College of Pharmaceutical Sciences
24900203 13 Development of Fluorescent Ligands for the Human 5-HT1A Receptor.EBI TBA
21520940 40 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.EBI VU University Medical Center
21495689 134 N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.EBI National Institute on Drug Abuse-Intramural Research Program
21353774 81 Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder.EBI Pfizer Inc.
21334902 46 Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands.EBI Chinese Academy of Sciences
21093272 126 Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.EBI Wyeth Research
21190848 61 1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.EBI Korea Research Institute of Chemical Technology
21185183 111 Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists.EBI Pfizer Inc.
20949929 63 Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.EBI Bristol Myers Squibb
20932009 127 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.EBI Wyeth Research
20888762 7 Identification of a red-emitting fluorescent ligand for in vitro visualization of human serotonin 5-HT(1A) receptors.EBI Università degli Studi di Bari A. Moro
20860381 61 Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.EBI Friedrich Alexander University
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
20801650 245 6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.EBI Pfizer Inc.
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20656482 36 Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.EBI University of Liège
20655748 92 Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.EBI Korea Research Institute of Chemical Technology
20662542 64 Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands.EBI University of Sydney
20620058 41 Smoothened antagonists for hair inhibition.EBI Pfizer Inc.
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
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, Ltd.
20363635 10 Identification of serotonin 5-HT1A receptor partial agonists in ginger.EBI Department of Chemistry and Applied Biosciences
20443629 38 The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.EBI Pfizer Global Research and Development
19939513 21 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists.EBI Chemical Diversity Research Institute
20346662 4 The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists.EBI Polish Academy of Sciences
20223662 174 Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.EBI Yangji Chemicals
20149649 133 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
19767206 9 Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.EBI National Institute of Mental Health
20031410 84 Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.EBI Pfizer Global Research and Development
20022748 4 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.EBI University of Li£ge
20170099 58 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.EBI Wyeth Research
20064720 44 Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity.EBI Wyeth Research
19954972 14 Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.EBI University of Sydney
19932965 80 Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT(1A) receptor and the serotonin transporter.EBI Wyeth Research
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
19773162 72 Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.EBI Arena Pharmaceuticals
19739674 39 Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists.EBI Universitat de Barcelona
19854053 152 Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.EBI Pfizer Global Research and Development
19783143 65 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
19719241 55 Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.EBI Wyeth Research
9182127 9 Perhydrogenation of tabersonine, ans Aspidiosperma indole alkaloid.EBI Université de Caen Basse-Normandle
 5 Two 5-HT1A Receptor-Interactive Tryptamine Derivatives from the Unripe Fruit of Evodia rutaecarpaEBI TBA
 49 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.EBI TBA
 26 Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptorEBI TBA
 45 Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonistsEBI TBA
 40 (Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonistsEBI TBA
 44 5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI TBA
 12 5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonistEBI TBA
 25 Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic propertiesEBI TBA
 16 4-Aminomethyl chromans: dependence of serotonin and dopamine binding upon aromatic ring substitutionEBI 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
19326916 43 Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.EBI Universidad Complutense de Madrid
19155177 52 Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.EBI Florida A&M University
19147349 35 Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists.EBI Pfizer Global Research and Development
19053888 114 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties.EBI Universita degli Studi di Bari
18800769 80 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.EBI Università degli Studi di Bari
18774793 85 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
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc.
18602261 65 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
18595716 142 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
18573659 47 Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.EBI GlaxoSmithKline
18571421 78 Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.EBI Wyeth Research
18511284 64 2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.EBI Wyeth Research
18507369 85 Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.EBI Theravance, Inc.
18456500 56 Preparation of piperazine derivatives as 5-HT7 receptor antagonists.EBI Ewha Womans University
17067154 27 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.EBI Uppsala University
18160289 119 1-Aminoindanes as novel motif with potential atypical antipsychotic properties.EBI Pfizer Global Research and Development
18053713 78 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
18032038 38 Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.EBI UCB Inflammation Discovery
17976986 80 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI Pfizer Global Research & Development
17804228 44 Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.EBI Lilly Research Laboratories
17672446 149 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
17571866 49 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
17524641 69 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI GlaxoSmithKline
17434731 51 Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.EBI Lilly SA
17407811 34 Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor.EBI Wyeth Research
17266201 13 Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.EBI Friedrich Alexander University
17064079 22 Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.EBI Università degli Studi di Bari
16759104 46 Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.EBI Friedrich Alexander University
16722631 87 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.
16677812 26 Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands.EBI Université Montpellier I et II
16621538 35 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
16563764 100 Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.EBI Friedrich-Alexander University
16458504 37 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.EBI Columbia University College of Physicians and Surgeons
16392816 113 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.EBI Alcon Research, Ltd.
16392798 46 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
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 Ltd
16332439 58 Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity.EBI Wyeth Research
16298130 32 Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5.EBI Lilly Research Laboratories
16219465 82 Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.EBI Abbott GmbH & Co. KG
16216506 31 3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands.EBI Università di Catania
16143528 213 Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI Columbia University College of Physicians and Surgeons
16139501 54 Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.EBI University of Erlangen-Nuremberg
15828846 47 Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.EBI Lundbeck Research USA, Inc.
15771448 187 Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI Johnson & Johnson Pharmaceutical Research & Development
15686885 28 Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.EBI Wyeth Research
15603958 77 N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.EBI Wyeth Research
15546719 38 Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.EBI Lilly Research Laboratories
15454211 19 Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity.EBI Wyeth Research
15267230 50 Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.EBI Uppsala University
15239661 120 Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.EBI Wyeth Research
15225707 42 Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.EBI University of Erlangen-Nuremberg
15109671 29 Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4.EBI Lilly Research Laboratories
15055991 265 Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor.EBI Recordati s.p.a.
15026055 22 The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.EBI ArQule Inc
14741267 43 Thiazoles and thiopyridines: novel series of high affinity h5HT(7) ligands.EBI Merck Sharp & Dohme Research Laboratories
14698193 43 Modulation of selective serotonin reuptake inhibitor and 5-HT1A antagonist activity in 8-aza-bicyclo[3.2.1]octane derivatives of 2,3-dihydro-1,4-benzodioxane.EBI Wyeth Research
14643338 124 Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI Virginia Commonwealth University
14611858 65 1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.EBI Neurogen Corporation
14592479 60 Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3.EBI Lilly Research Laboratories
12904082 20 New potential uroselective NO-donor alpha1-antagonists.EBI Università degli Studi di Torino
12877591 36 Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands.EBI Purdue University
12825944 184 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 Lilly Research Laboratories
12824042 64 Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2.EBI Lilly Research Laboratories
12749894 48 Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.EBI Lilly Research Laboratories
12643910 55 Identification of a novel series of selective 5-HT7 receptor antagonists.EBI GlaxoSmithKline
12161137 39 Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.EBI Friedrich-Alexander University
12109911 47 Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.EBI University Center for Pharmacy
11814784 53 Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors.EBI Wyeth-Ayerst Research Laboratories
11728188 53 trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.EBI Università Bari
11689074 112 N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.EBI Merck Sharp & Dohme Research Laboratories
11527728 56 New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.EBI Solvay Pharma
11514164 36 Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.EBI GlaxoSmithKline Pharmaceuticals
11448222 80 Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.EBI Istituto Chimico Farmaceutico e Tossicologico
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
11354362 18 Conformational analysis of tandospirone in aqueous solution: lead evolution of potent dopamine D4 receptor ligands.EBI Sumitomo Pharmaceuticals
11327592 9 1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors.EBI Wyeth-Ayerst Research
11311055 42 Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists.EBI Uppsala University
11277522 7 A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties.EBI Purdue University
11212112 24 Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.EBI Uppsala University
11101361 37 Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines.EBI Purdue University
11055342 21 N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.EBI Virginia Commonwealth University
10841797 110 Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI The R.W. Johnson Pharmaceutical Research Institute
10753471 64 Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.EBI Uppsala University
10715164 57 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.EBI Virginia Commonwealth University
10585208 212 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.EBI Merck Sharp & Dohme Research Laboratories
10498210 27 A new class of selective and potent inhibitors of neuronal nitric oxide synthase.EBI Pfizer Inc. Groton
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
10229627 11 Development of fluorine-18-labeled 5-HT1A antagonists.EBI National Institutes of Health
10052975 129 Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.EBI Merck, Sharp and Dohme Research Laboratories
9986723 29 N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.EBI Lilly Research Laboratories
9873746 13 Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.EBI Centre de Recherche Pierre Fabre
9871775 29 Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.EBI Centre de Recherche Pierre FABRE
9871581 12 Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.EBI Centre de Recherche Pierre FABRE
9857099 94 Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.EBI Synaptic Pharmaceutical Corporation
9632349 38 Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.EBI Pharmacia & Upjohn
9622542 119 Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.EBI Institut de Chimie Pharmaceutique
9397179 40 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.EBI Centre de Recherche Pierre FABRE
9357521 20 Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562).EBI Centre de Recherche Pierre FABRE
9057850 27 Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.EBI Pharmacia & Upjohn
9022796 57 5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.EBI Solvay Pharma
9016321 30 2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.EBI Neurogen Corporation
8960551 74 Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.EBI Centre de Recherche Pierre Fabre
8941384 51 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.EBI University of Groningen
8568822 80 Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.EBI Virginia Commonwealth University
8459396 37 Centrally acting serotonergic agents. Synthesis and structure-activity relationships of C-1- or C-3-substituted derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin.EBI Upjohn Laboratories
8340922 7 Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability.EBI Upjohn Laboratories
8097537 91 Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives.EBI Upjohn Laboratories
8071931 20 5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.EBI Medical College of Virginia/Virginia Commonwealth University
7731016 55 Quantitative binding site model generation: compass applied to multiple chemotypes targeting the 5-HT1A receptor.EBI Arris Pharmaceutical Corporation
7658443 5 Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.EBI Wellcome Research Laboratories
2918500 23 Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine.EBI University of Pennsylvania
1447752 28 Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.EBI Pfizer, Inc
1323682 61 Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.EBI Upjohn Company
27049670 47 Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1.BDB Max Planck Institute of Molecular Physiology
27136302 52 Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase.BDB University of Würzburg
26943478 16 Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.BDB Chulabhorn Research Institute
26518975 9 Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB Peking University
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
25384256 76 Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.BDB Vanderbilt University
25797804 18 An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.BDB Kyushu Institute of Technology
25462626 6 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
9647472 5 Pharmacological characterization of the human melatonin Mel1a receptor following stable transfection into NIH3T3 cells.BDB Universit&aagrove; degli Studi di Milano
9626023 49 Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs.BDB Dallas Department of Veterans Affairs Medical Center
9618903 37 Melatonin receptor pharmacology: toward subtype specificity.BDB King's College
8887981 72 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
8386236 11 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.
7518514 46 (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
2904784 109 Neuroleptic binding to human brain receptors: relation to clinical effects.BDB Mayo Clinic and Foundation
1836757 5 Molecular cloning and characterization of a rat brain cDNA encoding a 5-hydroxytryptamine1B receptor.BDB University of Heidelberg
19260711 12 Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily.BDB Bristol-Myers Squibb Company
18710209 14 Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid.BDB Eberhard-Karls-University Tuebingen
16302809 196 Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.BDB Rheinische Friedrich-Wilhelms-Universitat Bonn
12857114 102 High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II.BDB Uppsala University
15801830 127 Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4.BDB Pfizer