137 articles for thisTarget
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Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors.
Monash University (Parkville Campus)
Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor.
Bristol-Myers Squibb Research & Development
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.
Takeda Pharmaceutical
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.
Takeda Pharmaceutical
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.
Astrazeneca
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.
Takeda Pharmaceutical
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.
Bristol-Myers Squibb Research and Development
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414.
Boehringer Ingelheim Pharma
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908.
Boehringer Ingelheim Pharma
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.
Boehringer Ingelheim Pharma
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.
Bristol-Myers Squibb Research and Development
Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists.
Korea Research Institute of Chemical Technology
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.
Glaxosmithkline
Three-dimensional quantitative structure-activity relationship CoMSIA/CoMFA and LeapFrog studies on novel series of bicyclo [4.1.0] heptanes derivatives as melanin-concentrating hormone receptor R1 antagonists.
Universidad De Cartagena
Melanin concentrating hormone receptor 1 (MCHR1) antagonists-Still a viable approach for obesity treatment?
Leo Pharma
[¹8F]FE@SNAP-A new PET tracer for the melanin concentrating hormone receptor 1 (MCHR1): microfluidic and vessel-based approaches.
Medical University of Vienna
Synthesis, structure-activity relationship, and pharmacological studies of novel melanin-concentrating hormone receptor 1 antagonists 3-aminomethylquinolines: reducing human ether-a-go-go-related gene (hERG) associated liabilities.
Takeda Pharmaceutical
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.
Amgen
Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines.
Takeda Pharmaceutical
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: part 2.
Dr. Reddy'S Laboratories
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
Dr. Reddy'S Laboratories
An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors.
Prosidion
Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Neurocrine Biosciences
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
Neurocrine Biosciences
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.
Neurocrine Biosciences
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Taisho Pharmaceutical
4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1).
Korea Research Institute of Chemical Technology
Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2.
Amgen
Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Amgen
Melanin-concentrating hormone receptor 1 antagonists: synthesis, structure-activity relationship, docking studies, and biological evaluation of 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
Takeda Pharmaceutical
Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists.
Lundbeck Research Usa
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
Takeda Pharmaceutical
Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.
Korea Research Institute of Chemical Technology
Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition.
Amgen
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
Tsukuba Research Institute
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.
Amri
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.
Amri
Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.
Universidad De Navarra
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.
Alchemia
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
Dr. Reddy'S Laboratories
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
Arena Pharmaceuticals
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.
Astrazeneca R & D M£Lndal
Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists.
Tsukuba Research Institute
Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.
Astrazeneca R & D M£Lndal
Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R).
Tsukuba Research Institute
Homology modeling of MCH1 receptor and validation by docking/scoring and protein-aligned CoMFA.
University of Jordan
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
Tsukuba Research Institute
Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.
Johnson & Johnson Pharmaceutical R&D
Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.
Astrazeneca R&D MöLndal
Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening.
Molsoft
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Lundbeck Research Usa
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Lundbeck Research Usa
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.
Schering-Plough Research Institute
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.
Schering-Plough Research Institute
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.
Astrazeneca R&D MöLndal
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
Cerep
Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity.
University of Navarra
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Neurocrine Biosciences
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Abbott Laboratories
Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists.
Neurocrine Biosciences
Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.
Pharmacopeia Drug Discovery
The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.
Procter & Gamble Pharmaceuticals
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Abbott Laboratories
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Abbott Laboratories
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
Procter and Gamble Pharmaceuticals
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.
Glaxosmithkline
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.
Procter & Gamble Pharmaceuticals
MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.
Procter & Gamble Pharmaceuticals
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Procter & Gamble Pharmaceuticals
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Abbott Laboratories
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Merck Research Laboratories
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Merck Research Laboratories
Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
Schering-Plough Research Institute
Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.
Amgen
Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity.
Procter and Gamble Pharmaceuticals
Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.
Procter and Gamble Pharmaceuticals
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Neurocrine Biosciences
A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.
Neurocrine Biosciences
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
Schering-Plough Research Institute
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.
Schering-Plough Research Institute
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Millennium Pharmaceuticals
6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts.
7Tm Pharma
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Abbott Laboratories
Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.
Schering-Plough Research Institute
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Abbott Laboratories
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.
7Tm Pharma
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Abbott Laboratories
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.
Schering-Plough Research Institute
1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists.
Neurocrine Biosciences
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.
Pharmacopeia Drug Discovery
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.
Pharmacopeia Drug Discovery
Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Neurocrine Biosciences
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Abbott Laboratories
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Taisho Pharmaceutical
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
Schering-Plough Research Institute
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Abbott Laboratories
A screening library for peptide activated G-protein coupled receptors. 1. The test set.
Neurocrine Biosciences
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.
7Tm Pharma
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Abbott Laboratories
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.
Argenta Discovery
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
Argenta Discovery
Identification of a new small molecule chemotype of Melanin Concentrating Hormone Receptor-1 antagonists using pharmacophore-based virtual screening.
University of Science and Technology
Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs.
Hoffmann-La Roche
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
Glaxosmithkline
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.
Glaxosmithkline
Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review.
Indo-Soviet Friendship College of Pharmacy (Isfcp)
Preparation method for aromatic heterocyclic compound used as selective JAK3 and/or JAK1 kinase inhibitor and application of aromatic heterocyclic compound
Shenzhen Chipscreen Biosciences
Substituted benzimidazole and imidazopyridine compounds useful as CYP17 modulators
Bristol-Meyers Squibb
Rat alpha3/beta4 subtype of neuronal nicotinic acetylcholine receptor stably expressed in a transfected cell line: pharmacology of ligand binding and function.
Georgetown University
The core structures of roseophilin and the prodigiosin alkaloids define a new class of protein tyrosine phosphatase inhibitors.
Max-Planck-Institut FÜR Kohlenforschung
A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression.
Gpc Biotech