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265 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27997171 48 Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.EBI The University of Newcastle
12372505 120 Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.EBI Abbott Laboratories
12113835 176 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.EBI Abbott Laboratories
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
27866818 84 The discovery of quinoline based single-ligand human HEBI GlaxoSmithKline
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27643714 26 Identification of Ligand Binding Hot Spots of the Histamine HEBI Vrije Universiteit Amsterdam
27717652 275 Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI Florida A&M University
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
27007611 115 Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.EBI University of Regensburg
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
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26718844 55 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.EBI Friedrich-Alexander-Universit£t Erlangen-N£rnberg
25993395 19 Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.EBI Janssen Research and Development LLC
26191365 49 Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.EBI Novartis Institutes for BioMedical Research
25494650 8 CNS drug design: balancing physicochemical properties for optimal brain exposure.EBI Eli Lilly and Company
25827402 54 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.EBI Teva Global R & D.
25557493 109 Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI Jagiellonian University Collegium Medicum
25070422 126 Further evaluation of the tropane analogs of haloperidol.EBI Florida A&M University
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
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
25318072 48 Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.EBI Max Planck Institute of Psychiatry
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
24690494 92 Antagonists of the kappa opioid receptor.EBI The Scripps Research Institute
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
24650714 21 Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.EBI United Arab Emirates University
24365159 35 The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.EBI University of Missouri
24900633 11 Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.EBI Amgen Inc
24269482 35 Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.EBI GlaxoSmithKline
24161834 17 The discovery of the benzazepine class of histamine H3 receptor antagonists.EBI GlaxoSmithKline
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
23919353 8 Polypharmacology - foe or friend?EBI F. Hoffmann-La Roche Inc
24454993 1 Discovery of?2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.EBI University of Dundee
24035337 10 2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.EBI Virginia Commonwealth University
23981939 32 N-substituted 8-aminopentacyclo[,6).0(3,10).0(5,9)]undecanes ass receptor ligands with potential neuroprotective effects.EBI The University of Sydney
24611085 101 Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.EBI Sanford-Burnham Medical Research Institute
23816046 8 Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates.EBI Columbia University Medical Center
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
23591112 4 Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II).EBI Sanofi US
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£ degli Studi di Siena
23403082 28 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.EBI Broad Institute of MIT and Harvard
23558237 17 A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.EBI Griffin Discoveries BV
24900647 8 Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.EBI Goethe University
14667234 23 Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.EBI Vrije Universiteit Amsterdam
12443779 44 2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI Janssen-Cilag S.A.
21944853 41 Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.EBI University of Regensburg
20674357 66 Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.EBI GlaxoSmithKline
16408006 3 Linking agonist binding to histamine H1 receptor activation.EBI Vrije Universiteit Amsterdam
20409707 66 Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.EBI University of Regensburg
19791743 41 Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.EBI University of Regensburg
19524331 33 Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.EBI Johnson & Johnson Pharmaceutical Research & Development
19317445 53 N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.EBI University of Regensburg
19053770 68 Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.EBI Vrije Universiteit Amsterdam
18248991 323 New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.EBI GlaxoSmithKline
12657274 109 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott 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 S.A.
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 S.A.
12113836 162 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.EBI Abbott Laboratories
23142617 57 Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I.EBI AstraZeneca
23116889 88 Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: optimising in vivo clearance.EBI AstraZeneca
23099096 88 Novel azulene derivatives for the treatment of erectile dysfunction.EBI Friedrich-Alexander University
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI The University of Sydney
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
23641311 38 From a42 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.EBI TBA
23009245 53 Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI Sanford-Burnham Medical Research Institute
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
22931505 69 Chemokine receptor antagonists.EBI National Heart and Lung Institute
23031591 90 The discovery of CCR3/H1 dual antagonists with reduced hERG risk.EBI AstraZeneca
22793499 19 Shape-based reprofiling of FDA-approved drugs for the H1 histamine receptor.EBI University of Oxford
22694093 16 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI National Institute of Biological Sciences
23021991 153 Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.EBI AstraZeneca
21062081 47 Histamine H3 receptor as a drug discovery target.EBI TBA
22985961 99 Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI GlaxoSmithKline
22578490 35 Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI Cephalon Inc
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
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
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
20541426 46 Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.EBI Meiji Seika Kaisha, Ltd
20299215 49 Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.EBI Argenta Discovery Ltd
20188547 152 Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences Inc
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
17846138 26 Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.EBI Veterans Affairs Medical Center
19091563 79 Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.EBI Johann Wolfgang Goethe Universit£t
18950149 75 Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.EBI University of Regensburg
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
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
18077160 126 In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.EBI Abbott Laboratories
18023344 77 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration.EBI F. Hoffmann-La Roche Inc
17998160 101 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI F. Hoffmann-La Roche Inc
17407815 27 Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.EBI Janssen-Cilag S.A.
16821797 21 (R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.EBI Mitsubishi Pharma Corporation
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15771458 5 Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines.EBI Johnson & Johnson Pharmaceutical Research & Development
14998318 112 Selective optimization of side activities: another way for drug discovery.EBI Prestwick Chemical Inc.
12747773 13 Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.EBI Aventis Pharmaceuticals, Inc.
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 Research Laboratories
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI Universities of Lille
15203136 39 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
 52 Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activityEBI TBA
 24 1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonistsEBI TBA
22336245 72 Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.EBI Florida A&M University
22245230 128 Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI Florida A&M University
22153663 59 Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics.EBI Griffin Discoveries BV
22153347 111 Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia.EBI Neurocrine Biosciences Inc
22153342 60 Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI Cephalon Inc
22014551 33 Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI Cephalon Inc
22007643 25 Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.EBI VU University Amsterdam
21955944 39 Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).EBI Pfizer Inc
21788137 33 N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI The University of Sydney
20800486 16 Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences Inc
19443217 60 Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.EBI Chemical Diversity Research Institute
21555222 25 Molecular hybridization of 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (s) receptor ligands modulates off-target activity and subtype selectivity.EBI The University of Sydney
21470866 21 Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.EBI Dainippon Sumitomo Pharma Co., Ltd
21381763 52 The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.EBI GlaxoSmithKline
21232954 75 Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.EBI Neurocrine Biosciences Inc
21146989 46 Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI The University of Sydney
20942472 88 Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.EBI GlaxoSmithKline
20857909 176 Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.EBI University of Copenhagen
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20690643 68 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI Meiji Seika Kaisha, Ltd
20667729 86 Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI Evotec (UK) Ltd
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
20452213 65 Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.EBI Johnson & Johnson Pharmaceutical Research & Development
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
20347297 61 The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.EBI Neurocrine Biosciences Inc
20227880 144 Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences Inc
20153647 6 The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.EBI GlaxoSmithKline
19786348 261 Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.EBI F. Hoffmann-La Roche Inc
20045641 9 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.EBI Virginia Commonwealth University
20170186 49 1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.EBI GlaxoSmithKline
19945877 50 Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.EBI Chemical Diversity Research Institute
19773175 41 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.EBI Johann Wolfgang Goethe University
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
19660947 24 Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.EBI The Schering Plough Research Institute
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19553115 96 Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences Inc
19663387 29 Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences Inc
19520574 49 Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI Tsukuba Research Institute
19362477 24 Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists.EBI Dainippon Sumitomo Phrama. Co. Ltd
19553110 16 Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.EBI Tsukuba Research Institute
8496700 16 The Role of Receptor Binding in Drug DiscoveryEBI TBA
 76 Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activityEBI TBA
 32 The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI TBA
 44 5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonistsEBI TBA
 37 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
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
18952421 60 Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18841880 82 Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18817368 57 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI Merck Research Laboratories
18783208 11 Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.EBI National Institute of Mental Health
18768318 37 Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
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
18020391 12 From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.EBI F. Hoffmann-La Roche Inc
18020390 37 Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.EBI F. Hoffmann-La Roche Inc
17976986 80 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI Pfizer Inc
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
16942032 64 Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.EBI Hokkaido University
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
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
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
16143528 213 Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI Columbia University College of Physicians and Surgeons
16134937 154 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
15771448 187 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.
15771415 155 Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI Johnson & Johnson Pharmaceutical Research & Development
15686917 21 5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.EBI UCB Pharma SA
15634025 29 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.EBI Novo Nordisk A/S
15482930 22 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.EBI UCB Pharma SA
15125929 66 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.
15081022 20 5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.EBI UCB Pharma SA
14741266 203 Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.EBI Abbott Laboratories
12798320 64 A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.EBI Abbott Laboratories
12723960 58 Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.EBI Hokkaido University
12372500 108 Synthesis and evaluation of potent pyrrolidine H(3) antagonists.EBI Abbott Laboratories
11784148 81 Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI Pharmazeutisches Institut der Universität Freiburg
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
28797771 31 Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine HEBI Jagiellonian University Medical College
10956183 19 De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.EBI Synaptic Pharmaceutical Corporation
10937710 81 Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.EBI Merck & Co.
27331270 54 Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.EBI National Institute of Diabetes and Digestive and Kidney Diseases
31679973 18 Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and HEBI China Pharmaceutical University
32342685 325 Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI National Institute of Neurological Disorders and Stroke
31421966 20 Rasagiline derivatives combined with histamine HEBI Heinrich Heine University D£sseldorf
31021617 136 Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI University of Pennsylvania
30875219 254 Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI University of North Carolina at Chapel Hill
30605331 236 Design and in Vivo Characterization of AEBI Medical College of Wisconsin
31274307 24 Route to Prolonged Residence Time at the Histamine HEBI VU University Amsterdam
31185168 144 Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI RTI International
9857099 94 Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.EBI Synaptic Pharmaceutical Corporation
31913038 13 Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity.EBI University of Florida
31620230 283 3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI University of Minnesota Twin Cities
21075638 105 Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI Drug Discovery Laboratory AS
21044842 206 Histamine H4 receptor agonists.EBI University of Regensburg
18357976 53 Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.EBI Vrije Universiteit Amsterdam
15771452 49 N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.EBI Vrije Universiteit Amsterdam
12593665 188 Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.EBI Johannes Gutenberg-University of Mainz
30431269 41 Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.EBI Pfizer Inc.
30389290 146 Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI Texas Tech University Health Sciences Center
29324345 122 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
29730027 99 Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.EBI Jagiellonian University Medical College
29395980 84 Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.EBI University of Chinese Academy of Sciences
29656199 148 Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI University of Texas at Austin
29990431 138 Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets.EBI University of California San Francisco
29631962 252 Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI Phenex Pharmaceuticals AG
28774576 134 Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.EBI Xinjiang Technical Institute of Physics and Chemistry
28776992 110 Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI Northwestern University
28489950 119 Return of DEBI University of Nebraska Medical Center
1681106 27 Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.EBI Pfizer Inc
27666135 59 Rapid synthesis of flavone-based monoamine oxidase (MAO) inhibitors targeting two active sites using click chemistry.BDB Zhejiang University of Technology
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
26518975 9 Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB Peking University
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig
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
12388666 301 Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.BDB Institut de Recherches Servier
7925364 13 Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene.BDB Université Libre de Bruxelles
3828800 17 The characterization of [3H]sulpiride binding sites in rat striatal membranes.BDB St, Marianna University School of Medicine
17536795 118 Thiophene-anthranilamides as highly potent and orally available factor xa inhibitorsBDB Berlex Biosciences