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130 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors.EBI
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.EBI
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.EBI
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.EBI
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.EBI
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.EBI
Takeda Pharmaceutical
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.EBI
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.EBI
Boehringer Ingelheim Pharma
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908.EBI
Boehringer Ingelheim Pharma
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.EBI
Boehringer Ingelheim Pharma
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.EBI
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.EBI
Korea Research Institute Of Chemical Technology
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.EBI
Glaxosmithkline
Novel benzimidazole-based MCH R1 antagonists.EBI
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.EBI
Universidad De Cartagena
Melanin concentrating hormone receptor 1 (MCHR1) antagonists-Still a viable approach for obesity treatment?EBI
Leo Pharma
[¹8F]FE@SNAP-A new PET tracer for the melanin concentrating hormone receptor 1 (MCHR1): microfluidic and vessel-based approaches.EBI
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.EBI
Takeda Pharmaceutical
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI
Amgen
Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines.EBI
Takeda Pharmaceutical
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: part 2.EBI
Dr. Reddy'S Laboratories
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists.EBI
Dr. Reddy'S Laboratories
An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors.EBI
Prosidion
Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.EBI
Tsukuba Research Institute
Potent, selective MCH-1 receptor antagonists.EBI
Hoffmann-La Roche
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.EBI
Neurocrine Biosciences
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.EBI
Neurocrine Biosciences
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.EBI
Neurocrine Biosciences
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.EBI
Taisho Pharmaceutical
4-arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1).EBI
Korea Research Institute Of Chemical Technology
Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2.EBI
Amgen
Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.EBI
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.EBI
Takeda Pharmaceutical
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.EBI
Takeda Pharmaceutical
Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.EBI
Korea Research Institute Of Chemical Technology
Novel pyrrolidine melanin-concentrating hormone receptor 1 antagonists with reduced hERG inhibition.EBI
Amgen
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.EBI
Tsukuba Research Institute
5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.EBI
Amri
Tetrahydrocarboline analogs as MCH-1 antagonists.EBI
Amri
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.EBI
Amri
Building a MCHR1 homology model provides insight into the receptor-antagonist contacts that are important for the development of new anti-obesity agents.EBI
Universidad De Navarra
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.EBI
Alchemia
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.EBI
Dr. Reddy'S Laboratories
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.EBI
Arena Pharmaceuticals
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI
Tsukuba Research Institute
Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.EBI
Astrazeneca R & D M£Lndal
Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists.EBI
Tsukuba Research Institute
Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.EBI
Astrazeneca R & D M£Lndal
Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R).EBI
Tsukuba Research Institute
Homology modeling of MCH1 receptor and validation by docking/scoring and protein-aligned CoMFA.EBI
University Of Jordan
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.EBI
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.EBI
Johnson & Johnson Pharmaceutical R&D
Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.EBI
Astrazeneca R&D MöLndal
Discovery of novel chemotypes to a G-protein-coupled receptor through ligand-steered homology modeling and structure-based virtual screening.EBI
Molsoft
Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.EBI
Schering-Plough Research Institute
SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: taming hERG.EBI
Schering-Plough Research Institute
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists.EBI
Astrazeneca R&D MöLndal
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.EBI
Cerep
Novel series of substituted biphenylmethyl urea derivatives as MCH-R1 antagonists for the treatment of obesity.EBI
University Of Navarra
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).EBI
Neurocrine Biosciences
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.EBI
Abbott Laboratories
Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists.EBI
Neurocrine Biosciences
Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.EBI
Pharmacopeia Drug Discovery
The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.EBI
Procter & Gamble Pharmaceuticals
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.EBI
Abbott Laboratories
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.EBI
Abbott Laboratories
Quinazoline and benzimidazole MCH-1R antagonists.EBI
Argenta Discovery
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.EBI
Procter And Gamble Pharmaceuticals
6-(4-chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-based melanin-concentrating hormone receptor 1 antagonist.EBI
Glaxosmithkline
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.EBI
Glaxosmithkline
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.EBI
Procter & Gamble Pharmaceuticals
MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.EBI
Procter & Gamble Pharmaceuticals
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.EBI
Procter & Gamble Pharmaceuticals
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.EBI
Abbott Laboratories
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.EBI
Merck Research Laboratories
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.EBI
Merck Research Laboratories
Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.EBI
Schering-Plough Research Institute
Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.EBI
Amgen
Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity.EBI
Procter And Gamble Pharmaceuticals
Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents.EBI
Procter And Gamble Pharmaceuticals
Tetrahydroisoquinolines as MCH-R1 antagonists.EBI
Schering-Plough 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 1.EBI
Neurocrine Biosciences
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.EBI
Schering-Plough Research Institute
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.EBI
Schering-Plough Research Institute
Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.EBI
Schering-Plough Research Institute
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.EBI
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.EBI
Schering-Plough Research Institute
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.EBI
Millennium Pharmaceuticals
6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts.EBI
7Tm Pharma
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.EBI
Abbott Laboratories
Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.EBI
Schering-Plough Research Institute
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.EBI
Abbott Laboratories
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.EBI
7Tm Pharma
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.EBI
Abbott Laboratories
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.EBI
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.EBI
Neurocrine Biosciences
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.EBI
Pharmacopeia Drug Discovery
Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.EBI
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).EBI
Neurocrine Biosciences
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.EBI
Taisho Pharmaceutical
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.EBI
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.EBI
Abbott Laboratories
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.EBI
7Tm Pharma
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 3.EBI
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.EBI
Abbott Laboratories
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.EBI
Abbott Laboratories
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.EBI
Argenta Discovery
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.EBI
Argenta Discovery
Identification of a new small molecule chemotype of Melanin Concentrating Hormone Receptor-1 antagonists using pharmacophore-based virtual screening.EBI
University Of Science And Technology
Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs.EBI
Hoffmann-La Roche
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.EBI
Glaxosmithkline
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849.EBI
Glaxosmithkline
Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review.EBI
Indo-Soviet Friendship College Of Pharmacy (Isfcp)
Oxysterol-binding protein (OSBP)-related protein 4 (ORP4) is essential for cell proliferation and survival.BDB
Dalhousie University
Substituted furans as potent lipoxygenase inhibitors: Synthesis, in vitro and molecular docking studies.BDB
Csir-Indian Institute Of Chemical Biology
Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase.BDB
University Of Wurzburg
A Novel Inhibitor of the Obesity-Related Protein FTO.BDB
Basic Medical College Of Zhengzhou University
Synthesis and evaluation of novel marine bromopyrrole alkaloid-based derivatives as potential antidepressant agents.BDB
University Of Kwazulu-Natal
Differences in agonist/antagonist binding affinity and receptor transduction using recombinant human gamma-aminobutyric acid type A receptors.BDB
Merck Sharp And Dohme Research Laboratories
Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.BDB
The University Of Birmingham