PMID

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SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Glaxosmithkline

Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.

Glaxosmithkline

Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.

Eli Lilly

Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.

University of Kansas

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

Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.

The Alexander Shulgin Research Institute

Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.

City University of New York

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.

Glaxosmithkline

The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.

Smithkline Beecham Pharmaceuticals

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

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.

University of Caen Normandie

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

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

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.

Hunter College and The Graduate Center of The City University of New York

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

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

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

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

Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.

Hokkaido University

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

 

Bivalent indoles exhibiting serotonergic binding affinity

TBA

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

Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.

Glaxosmithkline

Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.

Theravance

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

Targeting σ

The University of Texas At Austin

Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.

High Point University

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

Discovery of Highly Potent Serotonin 5-HT

Northwestern University

Discovery of G Protein-Biased Ligands against 5-HT

Korea Institute of Science and Technology

Discovery of G Protein-Biased Antagonists against 5-HT

Korea Institute of Science and Technology

Structure-Activity Relationship of Heterocyclic P2Y

National Institute of Diabetes and Digestive and Kidney Diseases

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

Identification of a novel series of selective 5-HT7 receptor antagonists.

Glaxosmithkline

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.

Glaxosmithkline

Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.

Columbia University College of Physicians and Surgeons

Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge

University of Mississippi

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Virginia Commonwealth University

2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors.

Virginia Commonwealth University

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.

Merck Sharp & Dohme Research Laboratories

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D

National Institute of Neurological Disorders and Stroke

Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D

University of North Carolina At Chapel Hill

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.

Merck Sharp and Dohme Research Laboratories

3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT

University of Minnesota Twin Cities

Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.

Drug Discovery Laboratory

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.

Glaxosmithkline

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

Glaxosmithkline

Discovery of β-Arrestin Biased Ligands of 5-HT

Korea Institute of Science and Technology

Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products.

University of The Philippines

Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.

University of Texas At Austin

5-HT1 and 5-HT2 binding profiles of the serotonergic agents alpha-methylserotonin and 2-methylserotonin.

Virginia Commonwealth University

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.

Northwestern University

SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION

Genentech

6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes

Sprint Bioscience

Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

Ctxt

Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof

Beijing Tide Pharmaceutical

Trifluoromethylpropanamide derivatives

Hoffmann-La Roche

Compounds and compositions for inhibiting the activity of SHP2

Novartis

Piperidine oxadiazole and thiadiazole orexin receptor antagonists

Merck Sharp & Dohme

Fucosidase inhibitors

Horizon Orphan

N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders

Ogeda

Imidazole derivative having JNK inhibitory activity and use thereof

Samjin Pharmaceutical

Styryl quinazoline derivatives as pharmaceutically active agents

Vichem Chemie Kutató

Substituted 6,5-fused bicyclic heteroaryl compounds

Epizyme

Compounds useful as inhibitors of ATR kinase

Vertex Pharmaceuticals

Dihydropyrrolopyridine inhibitors of ROR-gamma

Vitae Pharmaceuticals

Pyrimidine PDE10 inhibitors

Merck Sharp & Dohme

Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.

The Scripps Research Institute

Identification of RIP1 kinase as a specific cellular target of necrostatins.

Tufts University

Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.

Ono Pharmaceutical

3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.

Wyeth Research

Biarylether amide quinolines as liver X receptor agonists.

Wyeth Research

Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.

Cnr

Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.

Purdue University

Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.

Yale University

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Bristol-Myers Squibb

Chalcones: a valid scaffold for monoamine oxidases inhibitors.

Sapienza University of Rome

Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.

Universita Del Piemonte Orientale

Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists.

Tanabe Research Laboratories Usa

Carbonic anhydrase inhibitors: synthesis and inhibition studies against mammalian isoforms I-XV with a series of 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides.

Istanbul University