117 articles for thisTarget
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Article Title
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Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Glaxosmithkline
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
Development of novel NK3 receptor antagonists with reduced environmental impact.
Kyoto University
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
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Euroscreen
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
Euroscreen
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.
Kyoto University
Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.
University of Montreal
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.
University of Montreal
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.
Merck Research Laboratories
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
University of Siena
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Bristol-Myers Squibb
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
Kyoto University
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.
Northeast Ohio Medical University
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.
Glaxosmithkline
New quinoline NK3 receptor antagonists with CNS activity.
Neuroscience Cedd Glaxosmithkline Research & Development
Cyclic peptides as selective tachykinin antagonists.
Merck Sharp and Dohme Research Laboratories
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists.
F. Hoffmann-La Roche
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.
Merck Sharp & Dohme Research Laboratories
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
Astrazeneca Pharmaceuticals
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).
Smithkline Beecham
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.
Cambridge University Forvie Site
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.
Smithkline Beecham
Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor.
Pierre and Marie Curie University
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
Glaxo Group Research
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Merck Sharp Laboratory
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
TBA
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
TBA
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
TBA
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.
Euroscreen
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists.
Astrazeneca Pharmaceuticals
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.
Northeastern Ohio Universities Colleges of Medicine and Pharmacy
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
F. Hoffmann-La Roche
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.
F. Hoffmann-La Roche
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
F. Hoffmann-La Roche
The dipeptide neurokinin-1 receptor antagonist S19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo
TBA
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
TBA
The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors
TBA
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
TBA
Alternative strategies towards the identification of chemical lead compounds by rational design
TBA
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes
TBA
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening.
TBA
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Merck Research Laboratories
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.
Schering-Plough Research Institute
Synthesis and evaluation of piperazinotriazoles. Discovery of a potent and orally bioavailable neurokinin-3 receptor inhibitor.
Binzhou Medical University
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Merck
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.
Merck Sharp & Dohme Research Laboratories
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.
Merck Research Laboratories
Cyclobutane derivatives as potent NK1 selective antagonists.
Schering-Plough Research Institute
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
Astrazeneca Pharmaceuticals
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.
Schering-Plough Research Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.
Sankyo
Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact.
Kyoto University
High affinity phenylglycinol-based NK1 receptor antagonists.
Merck Sharp and Dohme Research Laboratories
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.
Smithkline Beecham S.P.A. Milano
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
China Pharmaceutical University
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
Hebrew University of Jerusalem
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Merck Research Laboratories
Comparison of the conformation of active and nonactive backbone cyclic analogs of substance P as a tool to elucidate features of the bioactive conformation: NMR and molecular dynamics in DMSO and water.
Technische UniversitäT MüNchen
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.
Merck Sharp and Dohme Research Laboratories
Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
Menarini Ricerche
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.
Glaxo Wellcome Medicines Research Centre
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Phenex Pharmaceuticals
Pseudopeptide analogues of substance P and leucine enkephalinamide containing the psi (CH2O) modification: synthesis and biological activity.
Hebrew University of Jerusalem
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
Pfizer
NOVEL SUBSTITUTED PYRAZINE-CARBOXAMIDE DERIVATIVES
Boehringer Ingelheim International
Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.
Yale University
Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
Boehringer Ingelheim International
5-[3-[piperzin-1-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS 4 and 5 inhibitors for treating E.G. osteoarthritis
Galapagos
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
Albany Molecular Research
Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
Incyte
Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
Universidad Del PaíS Vasco
N-[3H]methylscopolamine labeling of non-M1, non-M2 muscarinic receptor binding sites in rat brain.
University of California
Switching between allosteric and dimerization inhibition of HIV-1 protease.
Purdue University
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Kochi Medical School
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Merck Research Laboratories
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
University of Tampere