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282 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28657744 167 Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.EBI University of Illinois At Chicago
28635286 207 Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HTEBI Bristol-Myers Squibb
27997171 48 Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.EBI The University of Newcastle
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
11459658 18 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.EBI Glaxosmithkline
10969987 63 1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.EBI Smithkline Beecham Pharmaceuticals
10969986 123 1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.EBI Smithkline Beecham Pharmaceuticals
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
27864071 116 Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HTEBI Arena Pharmaceuticals
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27933810 166 Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HTEBI National Institute of Diabetes and Digestive and Kidney Diseases
27717652 275 Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI Florida A&M University
27490827 24 Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.EBI Pfizer
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
27261181 45 New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.EBI City University of New York
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
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
26810316 29 Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.EBI Merck Research Laboratories
26739781 237 Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI The Alexander Shulgin Research Institute
26475518 19 Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI City University of New York
26421921 43 Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.EBI Glenmark Research Centre
26099069 15 Therapeutic Potential of 5-HT6 Receptor Agonists.EBI Universit£
26191370 34 Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.EBI National Institute of Diabetes and Digestive and Kidney Diseases
26227772 22 C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.EBI City University of New York
26270954 7 Synthesis and Characterization of 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC) and Its Analogues as Non-nitrogenous 5-HT2B Ligands.EBI Virginia Commonwealth University
25695425 62 Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.EBI City University of New York
25815155 21 Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.EBI University of Cambridge
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
25422861 78 In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.EBI National Institute of Diabetes and Digestive and Kidney Diseases
25703249 132 Novel 4-substituted-N,N-dimethyltetrahydronaphthalen-2-amines: synthesis, affinity, and in silico docking studies at serotonin 5-HT2-type and histamine H1 G protein-coupled receptors.EBI University of Florida
25699143 26 Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.EBI Pfizer
25070422 126 Further evaluation of the tropane analogs of haloperidol.EBI Florida A&M University
24916029 42 Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2.EBI Astellas Pharma
24863744 15 DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.EBI University of Missouri
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
24900864 21 Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.EBI Pfizer
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
24800940 146 Identification of a new selective dopamine D4 receptor ligand.EBI Florida A&M University
24279689 56 Prostanoid receptor EP2 as a therapeutic target.EBI Emory University
24704027 31 Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists.EBI Cephalon
24690494 92 Antagonists of the kappa opioid receptor.EBI The Scripps Research Institute
24900826 22 Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects.EBI Therachem Research Medilab (India)
24900821 5 Quinoline Derivatives as 5-HT6 Receptor PET Ligands.EBI Dart Neuroscience
16730983 165 Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.EBI Glaxosmithkline
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
23560650 46 Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selectives1 receptor ligands.EBI Esteve
23374867 40 Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.EBI Eli Lilly
23177783 130 Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.EBI Bristol-Myers Squibb Research and Development
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
23606928 14 Synthesis of novel analogs of cabergoline: improving cardiovascular safety by removing 5-HT2B receptor agonism.EBI University of Minnesota
20674357 66 Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.EBI Glaxosmithkline
19146417 70 The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.EBI Glaxosmithkline
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
16168649 65 A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.EBI Glaxosmithkline
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
23084435 17 Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.EBI Savannah State University
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI The University of Sydney
23641311 38 From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.EBI TBA
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£
22784008 100 Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).EBI Esteve
22664127 19 Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines-Synthesis and 'structure-activity' relationship.EBI Chemical Diversity Research Institute
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
22694093 16 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.EBI National Institute of Biological Sciences
22386241 46 Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.EBI Sk Biopharmaceuticals
22313242 146 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.EBI Pfizer
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
22778800 24 Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.EBI TBA
22465637 48 4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators.EBI Lundbeck Research Usa
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
20727749 17 Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).EBI University of Sydney
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
20560595 21 (3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.EBI Chemical Diversity Research Institute
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
19720528 54 Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.EBI Wyeth Research
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
18083579 33 Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.EBI Astellas Pharma
18035544 52 Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.EBI Astellas Pharma
18282705 69 2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
17998160 101 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.EBI F. Hoffmann-La Roche
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes For Biomedical Research
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
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
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 Eli Lilly
15203136 39 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
22226656 75 Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.EBI Cephalon
22153937 52 Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists.EBI Cephalon
22001031 6 Usabamycins A-C: new anthramycin-type analogues from a marine-derived actinomycete.EBI Nippon Suisan Kaisha
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
21871797 33 Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazines¿? receptor ligands.EBI The University of Sydney
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
21907583 48 CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.EBI University of South Florida
21195614 56 Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.EBI Pfizer
21333408 21 2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: new series of highly potent and specific serotonin 5-HT6 receptor antagonists.EBI Chemical Diversity Research Institute
21028889 7 Pulicatins A-E, neuroactive thiazoline metabolites from cone snail-associated bacteria.EBI University of Utah
21093272 126 Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.EBI Wyeth Research
21146989 46 Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI The University of Sydney
21146986 50 Novel 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohepta[f]indene analogues as potent and selective 5-HT(2C) agonists for the treatment of metabolic disorders.EBI Evotec
20958049 12 Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.EBI University of North Carolina At Chapel Hill
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
20812727 157 Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI National Institute of Mental Health
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20692833 41 N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.EBI Csiro Molecular and Health Technologies
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
20455563 49 Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.EBI Arena Pharmaceuticals
20207539 15 Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists.EBI Chemical Diversity Research Institute
20202843 40 Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.EBI Pfizer
19786348 261 Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists.EBI F. Hoffmann-La Roche
20022752 94 Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.EBI Bristol-Myers Squibb
20170099 58 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.EBI Wyeth Research
19914063 84 Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.EBI Pfizer
19646882 72 Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
19773162 72 Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.EBI Arena Pharmaceuticals
19716297 45 Design and synthesis of pyridazinone-based 5-HT(2C) agonists.EBI Pfizer
19692241 36 Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists.EBI Pfizer
19646865 45 Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.EBI Pfizer
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
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
19307114 73 A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.EBI Boehringer Ingelheim Pharmaceuticals
19284718 191 Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.EBI University of Illinois At Chicago
19269173 81 7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.EBI Pfizer
18701276 97 Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI Merck Research Laboratories
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen
18621528 133 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.EBI Pfizer
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
18557608 108 Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors.EBI Wyeth Research
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
17315987 268 Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.EBI Pharmaceutical Research Institute
17178222 29 Quinazoline and benzimidazole MCH-1R antagonists.EBI Argenta Discovery
16844377 40 New spiro-piperidines as 5-HT2B receptor antagonists.EBI Hopital Saint-Louis
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
16546379 30 The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists.EBI Athersys
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
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
16257207 96 Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.EBI Vernalis
16061378 87 SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.EBI Organix
15975787 39 Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.EBI Vernalis Research
15713408 96 Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity.EBI Arena Pharmaceuticals
15225734 10 Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.EBI Argenta Discovery
15109661 21 Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.EBI Wyeth Research
15081042 84 Indoline derivatives as 5-HT(2C) receptor agonists.EBI Vernalis Research
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 Eli Lilly
12643910 55 Identification of a novel series of selective 5-HT7 receptor antagonists.EBI Glaxosmithkline
12502367 17 New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.EBI Université
11514164 36 Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.EBI Glaxosmithkline
32527538 30 Azetidine-based selective glycine transporter-1 (GlyT1) inhibitors with memory enhancing properties.EBI Dart Neuroscience
32551645 51 2-Arylbenzo[EBI University of Oxford
31952960 234 Discovery of a lead series of potent benzodiazepine 5-HTEBI Arena Pharmaceuticals
32227883 40 Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge EBI University of Mississippi
27410258 21 South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.EBI National Institute of Diabetes and Digestive and Kidney Diseases
27381086 68 Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines.EBI Pfizer
30622024 9 Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HTEBI Csir-Central Drug Research Institute (Csir-Cdri)
30597325 17 Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (?EBI Memorial Sloan Kettering Cancer Center
10737744 146 Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.EBI Smithkline Beecham Pharmaceuticals
31298539 18 Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68).EBI Icahn School of Medicine At Mount Sinai
32342685 325 Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI National Institute of Neurological Disorders and Stroke
31021617 136 Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI University of Pennsylvania
31112891 30 Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.EBI National University of Ireland Galway
30875219 254 Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI University of North Carolina At Chapel Hill
10090793 12 Thieno[3,2-b]- and thieno[2,3-b]pyrrole bioisosteric analogues of the hallucinogen and serotonin agonist N,N-dimethyltryptamine.EBI Purdue University
30545651 27 Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HTEBI Harvard Medical School
30605331 236 Design and in Vivo Characterization of AEBI Medical College of Wisconsin
31537425 11 Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.EBI Jagiellonian University Medical College
31185168 144 Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI Rti International
31445232 78 Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HTEBI University of Illinois At Chicago
31199640 50 Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.EBI Astrazeneca
31743642 198 4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual ?-Opioid Receptor Agonists and ?EBI Esteve Pharmaceuticals
9857084 11 A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor.EBI Purdue University
9836617 30 Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives.EBI Purdue University
30826188 25 Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.EBI University of Science & Technology (Ust)
9622555 25 Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity.EBI Purdue University
9301661 32 Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives.EBI Purdue University
31586817 96 Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.EBI Medical University of Warsaw
29620897 5 Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HTEBI TBA
31620230 283 3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI University of Minnesota Twin Cities
8709129 18 Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups.EBI Purdue University
26565745 165 Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI Janssen Pharmaceutica
25281269 35 Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.EBI Astellas Pharma
23683593 231 Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.EBI Bristol-Myers Squibb Research and Development
21075638 105 Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI Drug Discovery Laboratory
18095642 111 Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.EBI Arena Pharmaceuticals
17129726 121 3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.EBI Glaxosmithkline
17880057 131 Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.EBI Solvay Pharma
17079142 42 5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.EBI Glaxosmithkline
17074479 96 Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation.EBI Glaxosmithkline Medicine Research Centre
15887956 77 Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI Glaxosmithkline
16002289 65 Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.EBI Glaxosmithkline
9572885 118 Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.EBI Smithkline Beecham Pharmaceuticals
30344910 20 Exploring Halogen Bonds in 5-Hydroxytryptamine 2B Receptor-Ligand Interactions.EBI National Institute of Biological Sciences
30389290 146 Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI Texas Tech University Health Sciences Center
29407591 276 Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.EBI Jagiellonian University Medical College
30258529 34 5-HTEBI Usona Institute
30028132 135 Discovery of ?-Arrestin Biased Ligands of 5-HTEBI Korea Institute of Science and Technology
28745513 309 Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.EBI University of The Philippines
29767967 74 Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI National Institute of Diabetes and Digestive and Kidney Diseases
29656199 148 Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI University of Texas At Austin
29906396 10 Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).EBI Janssen Pharmaceutical Companies of Johnson & Johnson
28947947 112 Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.EBI Novartis Institutes For Biomedical Research
29631962 252 Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI Phenex Pharmaceuticals
28958623 35 Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HEBI Glaxosmithkline
28776992 110 Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.EBI Northwestern University
28636348 9 Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.EBI National Institute of Diabetes and Digestive and Kidney Diseases
28389149 56 Discovery of selective, orally bioavailable, N-linked arylsulfonamide NaEBI Department of Discovery Chemistry Merck
27136302 52 Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase.BDB University of Wurzburg
27064299 8 Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.BDB Broad Institute
26851737 36 One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.BDB University of Karachi
26637946 27 Benzimidazole derivatives as new a-glucosidase inhibitors and in silico studies.BDB Universiti Teknologi Mara (Uitm)
26451651 20 Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast a-glucosidase, acetylcholinesterase and butyrylcholinesterase.BDB Gc University
26077890 33 Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.BDB Tehran University of Medical Sciences
26364932 22 Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.BDB University of North Carolina At Chapel Hill
11579444 23 Resolution, configurational assignment, and enantiopharmacology at glutamate receptors of 2-amino-3-(3-carboxy-5-methyl-4-isoxazolyl)propionic acid (ACPA) and demethyl-ACPA.BDB The Royal Danish School of Pharmacy
9536007 23 Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach.BDB University of Bonn
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