95 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Minnesota
N-benzoyl-1,5-benzothiazepine and its S-oxide as vasopressin receptor ligands: insight into the active stereochemistry around the seven-membered ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Teikyo University
Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
F. Hoffmann-La Roche
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Strasburg
New, potent, and selective peptidic oxytocin receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ferring Research Institute
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 2. Synthesis, chirality, and pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
The College of New Jersey
Colloidal aggregation causes inhibition of G protein-coupled receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of North Carolina At Chapel Hill
Optimisation of pharmacokinetic properties to afford an orally bioavailable and selective V1A receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Msd
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Strasburg
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Synthesis and evaluation of C-11, F-18 and I-125 small molecule radioligands for detecting oxytocin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Emory University
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Strasburg
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Schering-Plough Research Institute
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
The discovery of GSK221149A: a potent and selective oxytocin antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Glaxosmithkline
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Institute Genomics Functional (Igf)
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Serono Pharmaceutical Research Institute
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medical College of Ohio
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Montpellier
Synthesis and evaluation of nonpeptide substituted spirobenzazepines as potent vasopressin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson and Johnson Pharmaceutical Research and Development
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Lehigh University
Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
New, potent, selective, and short-acting peptidic V1a receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ferring Research Institute
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Abbott Laboratories
Identification and optimisation of novel sulfonamide, selective vasopressin V1B receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Msd
Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Montpellier
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Msd
Spiroindolones, a potent compound class for the treatment of malaria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Swiss Tropical and Public Health Institute
Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Ligand Pharmaceuticals
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Vantia
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Pfizer
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Columbia University College of Physicians and Surgeons
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth Research
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson and Johnson Pharmaceutical Research and Development
Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Central Pharmaceutical Research Institute
2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson & Johnson Pharmaceutical Research & Development
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Johnson and Johnson Pharmaceutical Research and Development
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Otsuka Pharmaceutical
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Yamanouchi Pharmaceutical
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Otsuka Pharmaceutical
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth-Ayerst Research
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth-Ayerst Research
4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth-Ayerst Research
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Fluorescent pseudo-peptide linear vasopressin antagonists: design, synthesis, and applications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
University of Montpellier
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Shanghai Hengrui Pharmaceutical
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Wyeth-Ayerst Research
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Calibr At The Scripps Research Institute
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Merck Research Laboratories
Dicarbavasopressin antagonist analogues exhibit reduced in vivo agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Smith Kline & French Laboratories
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Umr7200 Cnrs/Universit£
A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Smith Kline & French Laboratories
Structure-activity relationships of novel vasopressin antagonists containing C-terminal diaminoalkanes and (aminoalkyl)guanidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Smith Kline & French Laboratories
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Imperial College
Tolvaptan-Type Vasopressin Receptor Ligands: Important Role of Axial Chirality in the Active Form.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Teikyo University
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Yogi Vemana University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Leipzig
New natural cholinesterase inhibiting and calcium channel blocking quinoline alkaloids.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of Karachi
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Cardiff University
The motilin pharmacophore in CHO cells expressing the human motilin receptor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Katholieke Universiteit Leuven
Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
University of North Carolina At Chapel Hill
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Merck Frosst Centre For Therapeutic Research