The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28657744 |
167 |
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
University of Illinois At Chicago |
28635286 |
207 |
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT |
Bristol-Myers Squibb |
27997171 |
48 |
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. |
The University of Newcastle |
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. |
Smithkline Beecham Pharmaceuticals |
2157007 |
9 |
Synthesis and alpha 2-adrenoceptor effects of substituted catecholimidazoline and catecholimidazole analogues in human platelets. |
Ohio State University |
7120280 |
9 |
Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety. |
TBA |
12392747 |
36 |
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Glaxosmithkline |
11992776 |
70 |
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists. |
Glaxosmithkline |
11266169 |
27 |
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor. |
Smithkline Beecham Pharmaceuticals |
11597412 |
116 |
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor. |
Glaxosmithkline |
11459658 |
18 |
1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. |
Glaxosmithkline |
11392544 |
11 |
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
Ucb Pharma |
10969987 |
63 |
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists. |
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. |
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-CH |
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. |
Eli Lilly |
27864071 |
116 |
Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT |
Arena Pharmaceuticals |
27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
27933810 |
166 |
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT |
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. |
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. |
Pfizer |
27364609 |
230 |
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
Florida A&M University |
27312422 |
219 |
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. |
Florida A&M University |
27261181 |
45 |
New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands. |
City University of New York |
26876931 |
36 |
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket. |
Abbott Healthcare Products |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
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. |
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. |
National Institute of Biological Sciences, Beijing |
26852005 |
82 |
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists. |
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. |
Merck Research Laboratories |
26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
26475518 |
19 |
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor. |
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. |
Glenmark Research Centre |
26099069 |
15 |
Therapeutic Potential of 5-HT6 Receptor Agonists. |
Universit£ |
26191370 |
34 |
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy. |
National Institute of Diabetes and Digestive and Kidney Diseases |
26227772 |
22 |
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity. |
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. |
Virginia Commonwealth University |
25695425 |
62 |
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
City University of New York |
25815155 |
21 |
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. |
University of Cambridge |
25633969 |
96 |
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
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. |
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. |
University of Florida |
25699143 |
26 |
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists. |
Pfizer |
25070422 |
126 |
Further evaluation of the tropane analogs of haloperidol. |
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. |
Astellas Pharma |
24863744 |
15 |
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
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. |
Novartis Institutes For Biomedical Research |
24900864 |
21 |
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. |
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. |
Pfizer |
24800940 |
146 |
Identification of a new selective dopamine D4 receptor ligand. |
Florida A&M University |
24279689 |
56 |
Prostanoid receptor EP2 as a therapeutic target. |
Emory University |
24704027 |
31 |
Lactam and oxazolidinone derived potent 5-hydroxytryptamine 6 receptor antagonists. |
Cephalon |
24690494 |
92 |
Antagonists of the kappa opioid receptor. |
The Scripps Research Institute |
24900826 |
22 |
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects. |
Therachem Research Medilab (India) |
24900821 |
5 |
Quinoline Derivatives as 5-HT6 Receptor PET Ligands. |
Dart Neuroscience |
16730983 |
165 |
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation. |
Glaxosmithkline |
23477943 |
51 |
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression. |
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. |
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. |
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. |
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. |
Novartis Pharma |
23606928 |
14 |
Synthesis of novel analogs of cabergoline: improving cardiovascular safety by removing 5-HT2B receptor agonism. |
University of Minnesota |
20674357 |
66 |
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders. |
Glaxosmithkline |
19146417 |
70 |
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor. |
Glaxosmithkline |
18829312 |
64 |
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity. |
Glaxosmithkline |
18433113 |
124 |
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
Glaxosmithkline |
16168649 |
65 |
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists. |
Glaxosmithkline |
11229746 |
6 |
First tricyclic oximino derivatives as 5-HT3 ligands. |
Universit£ |
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). |
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. |
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). |
The University of Sydney |
23641311 |
38 |
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design. |
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. |
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). |
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. |
Chemical Diversity Research Institute |
22845053 |
100 |
Structure-functional selectivity relationship studies ofß-arrestin-biased dopamine D2 receptor agonists. |
University of North Carolina At Chapel Hill |
22738628 |
38 |
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors. |
University of Li£Ge |
22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
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. |
Sk Biopharmaceuticals |
22313242 |
146 |
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. |
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. |
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. |
TBA |
22465637 |
48 |
4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators. |
Lundbeck Research Usa |
21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
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. |
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). |
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. |
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. |
Chemical Diversity Research Institute |
19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
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. |
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. |
Purdue University |
18083579 |
33 |
Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. |
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. |
Astellas Pharma |
18282705 |
69 |
2-Alkyl-4-aryl-pyrimidine fused heterocycles as selective 5-HT2A antagonists. |
Johnson & Johnson Pharmaceutical Research and Development |
17998160 |
101 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. |
F. Hoffmann-La Roche |
16451077 |
86 |
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. |
Pfizer |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
15482914 |
25 |
Azaadamantane benzamide 5-HT4 agonists: gastrointestinal prokinetic SC-54750. |
Pfizer |
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. |
Alcon Research |
12825922 |
207 |
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
Virginia Commonwealth 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). |
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. |
Eli Lilly |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
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. |
Cephalon |
22153937 |
52 |
Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists. |
Cephalon |
22001031 |
6 |
Usabamycins A-C: new anthramycin-type analogues from a marine-derived actinomycete. |
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. |
Vu University Medical Center |
21871797 |
33 |
Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazines¿? receptor ligands. |
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. |
Lundbeck Research Usa |
21907583 |
48 |
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
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. |
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. |
Chemical Diversity Research Institute |
21028889 |
7 |
Pulicatins A-E, neuroactive thiazoline metabolites from cone snail-associated bacteria. |
University of Utah |
21093272 |
126 |
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. |
Wyeth Research |
21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
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. |
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. |
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. |
Bristol-Myers Squibb |
20932009 |
127 |
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. |
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. |
National Institute of Mental Health |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20692833 |
41 |
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B. |
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. |
University of Sydney |
20620058 |
41 |
Smoothened antagonists for hair inhibition. |
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. |
Arena Pharmaceuticals |
20207539 |
15 |
Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
20202843 |
40 |
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity. |
Pfizer |
19786348 |
261 |
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists. |
F. Hoffmann-La Roche |
20022752 |
94 |
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. |
Bristol-Myers Squibb |
20170099 |
58 |
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. |
Wyeth Research |
19914063 |
84 |
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. |
Pfizer |
19646882 |
72 |
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
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. |
Arena Pharmaceuticals |
19716297 |
45 |
Design and synthesis of pyridazinone-based 5-HT(2C) agonists. |
Pfizer |
19692241 |
36 |
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists. |
Pfizer |
19646865 |
45 |
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence. |
Pfizer |
19783143 |
65 |
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead. |
Novartis Institutes For Biomedical Research |
| 40 |
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists |
TBA |
| 21 |
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamides |
TBA |
| 32 |
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) |
TBA |
| 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
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. |
TBA |
| 39 |
Novel conformationally restricted aromatic piperidines as selective sigma receptor ligands |
TBA |
| 54 |
Novel ether derivatives of alkyl piperidines as potential sigma / 5HT2 antipsychotic agents |
TBA |
19329329 |
183 |
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET. |
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. |
Boehringer Ingelheim Pharmaceuticals |
19284718 |
191 |
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
University of Illinois At Chicago |
19269173 |
81 |
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization. |
Pfizer |
18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
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. |
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. |
Florida A&M University |
18573659 |
47 |
Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. |
Glaxosmithkline |
18557608 |
108 |
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors. |
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. |
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. |
Pharmaceutical Research Institute |
17178222 |
29 |
Quinazoline and benzimidazole MCH-1R antagonists. |
Argenta Discovery |
16844377 |
40 |
New spiro-piperidines as 5-HT2B receptor antagonists. |
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. |
Predix Pharmaceuticals |
16546379 |
30 |
The identification of pyrimidine-diazabicyclo[3.3.0]octane derivatives as 5-HT2C receptor agonists. |
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. |
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. |
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. |
F. Hoffmann-La Roche |
16257207 |
96 |
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. |
Vernalis |
16061378 |
87 |
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. |
Organix |
15975787 |
39 |
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists. |
Vernalis Research |
15713408 |
96 |
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
Arena Pharmaceuticals |
15225734 |
10 |
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists. |
Argenta Discovery |
15149647 |
10 |
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist. |
Pfizer |
15109661 |
21 |
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor. |
Wyeth Research |
15081042 |
84 |
Indoline derivatives as 5-HT(2C) receptor agonists. |
Vernalis Research |
14611858 |
65 |
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands. |
Neurogen |
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. |
Eli Lilly |
12643910 |
55 |
Identification of a novel series of selective 5-HT7 receptor antagonists. |
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. |
Université |
11514164 |
36 |
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists. |
Glaxosmithkline |
32527538 |
30 |
Azetidine-based selective glycine transporter-1 (GlyT1) inhibitors with memory enhancing properties. |
Dart Neuroscience |
32551645 |
51 |
2-Arylbenzo[ |
University of Oxford |
31952960 |
234 |
Discovery of a lead series of potent benzodiazepine 5-HT |
Arena Pharmaceuticals |
32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
27410258 |
21 |
South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase. |
National Institute of Diabetes and Digestive and Kidney Diseases |
10853650 |
36 |
Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. |
Yoshitomi Pharmaceutical Industries |
27381086 |
68 |
Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
Pfizer |
30622024 |
9 |
Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT |
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 (? |
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. |
Smithkline Beecham Pharmaceuticals |
31298539 |
18 |
Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
Icahn School of Medicine At Mount Sinai |
32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
31021617 |
136 |
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D |
University of Pennsylvania |
31112891 |
30 |
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity. |
National University of Ireland Galway |
30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
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. |
Purdue University |
30545651 |
27 |
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
Harvard Medical School |
30605331 |
236 |
Design and in Vivo Characterization of A |
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. |
Jagiellonian University Medical College |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
31445232 |
78 |
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
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. |
Astrazeneca |
31743642 |
198 |
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual ?-Opioid Receptor Agonists and ? |
Esteve Pharmaceuticals |
9857084 |
11 |
A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor. |
Purdue University |
9836617 |
30 |
Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives. |
Purdue University |
30826188 |
25 |
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
University of Science & Technology (Ust) |
9622555 |
25 |
Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity. |
Purdue University |
9301661 |
32 |
Dihydrobenzofuran analogues of hallucinogens. 4. Mescaline derivatives. |
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. |
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-HT |
TBA |
31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
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. |
Purdue University |
26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
25281269 |
35 |
Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists. |
Astellas Pharma |
23683593 |
231 |
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists. |
Bristol-Myers Squibb Research and Development |
21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
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. |
Arena Pharmaceuticals |
17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
17079142 |
42 |
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation. |
Glaxosmithkline |
17074479 |
96 |
Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation. |
Glaxosmithkline Medicine Research Centre |
15887956 |
77 |
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. |
Glaxosmithkline |
16002289 |
65 |
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. |
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. |
Smithkline Beecham Pharmaceuticals |
30344910 |
20 |
Exploring Halogen Bonds in 5-Hydroxytryptamine 2B Receptor-Ligand Interactions. |
National Institute of Biological Sciences |
30389290 |
146 |
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. |
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. |
Jagiellonian University Medical College |
30258529 |
34 |
5-HT |
Usona Institute |
30028132 |
135 |
Discovery of ?-Arrestin Biased Ligands of 5-HT |
Korea Institute of Science and Technology |
28745513 |
309 |
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products. |
University of The Philippines |
29767967 |
74 |
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y |
National Institute of Diabetes and Digestive and Kidney Diseases |
29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
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). |
Janssen Pharmaceutical Companies of Johnson & Johnson |
28947947 |
112 |
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. |
Novartis Institutes For Biomedical Research |
29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
28958623 |
35 |
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H |
Glaxosmithkline |
28776992 |
110 |
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. |
Northwestern University |
28636348 |
9 |
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle. |
National Institute of Diabetes and Digestive and Kidney Diseases |
1674541 |
24 |
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity. |
Harvard Medical School |
1323682 |
61 |
Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor. |
Upjohn |
28389149 |
56 |
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na |
Department of Discovery Chemistry Merck |
27136302 |
52 |
Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase. |
University of Wurzburg |
27064299 |
8 |
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile. |
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. |
University of Karachi |
26637946 |
27 |
Benzimidazole derivatives as new a-glucosidase inhibitors and in silico studies. |
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. |
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. |
Tehran University of Medical Sciences |
26364932 |
22 |
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity. |
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. |
The Royal Danish School of Pharmacy |
9536007 |
23 |
Characterization of I2 imidazoline and sigma binding sites in the rat and human stomach. |
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. |
Whitby Research |