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255 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
12372504 15 Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands.EBI F. Hoffmann-La Roche AG
12182851 15 Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.EBI F. Hoffmann-La Roche AG
27876250 60 Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI Jagiellonian University Medical College
28105278 10 Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.EBI Mossakowski Medical Research Centre Polish Academy of Sciences
26713106 59 Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.EBI Vrije Universiteit Brussel
26988801 55 Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI Jagiellonian University Medical College
26048800 55 Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.EBI Bristol-Myers Squibb Co.
25738882 210 Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).EBI Euroscreen SA
25494650 8 CNS drug design: balancing physicochemical properties for optimal brain exposure.EBI Eli Lilly and Company
25544687 60 Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.EBI Vrije Universiteit Brussel
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
25516784 12 Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.EBI Uppsala University
24900878 40 Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.EBI Universit£ de Montr£al
12565946 51 Discovery of orally bioavailable NK1 receptor antagonists.EBI UCB Pharma
24507922 20 Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.EBI Bristol-Myers Squibb Company
24374277 41 Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.EBI Universit£ de Montr£al
24900633 11 Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.EBI Amgen Inc.
24075145 17 Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.EBI GlaxoSmithKline Medicines Research Centre
23899615 18 Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.EBI University of Arizona
23808489 11 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.EBI Merck Research Laboratories
23735006 17 Constrained H-Phe-Phe-NH2 analogues with high affinity to the substance P 1-7 binding site and with improved metabolic stability and cell permeability.EBI Uppsala University
23582449 20 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.EBI Institute of Organic Synthesis
23466604 36 Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.EBI Universit£ degli Studi di Siena
23403082 28 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.EBI Broad Institute of MIT and Harvard
23477943 51 Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.EBI Bristol-Myers Squibb Company
23253443 135 Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.EBI Bristol-Myers Squibb Research and Development
23281966 8 Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.EBI AstraZeneca
7473572 28 Quantitative structure-activity relationships (QSARs) of N-terminus fragments of NK1 tachykinin antagonists: a comparison of classical QSARs and three-dimensional QSARs from similarity matrices.EBI Cambridge University Forvie Site
12372532 45 Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.EBI UCB Pharma SA
21974957 27 Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.EBI GlaxoSmithKline Medicines Research Centre
19963378 11 Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
19388677 10 Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.EBI GlaxoSmithKline Medicines Research Centre
19473027 21 Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.EBI National Institute of Neuroscienc
16289817 23 Piperazinyl oxime ethers as NK-1 receptor antagonists.EBI Solvay Pharma
12431064 43 Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-[2-[(3-substituted)-1-azetidinyl]ethyl]-2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor.EBI Pfizer Inc.
9733486 91 Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.EBI Washington University
11755367 38 First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.EBI UCB Pharma SA
22574973 36 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.EBI F. Hoffmann-La Roche AG
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
21421318 25 Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.EBI Universit£ degli Studi di Siena
20875743 90 Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relaEBI Pfizer Inc.
20684563 176 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI H. Lundbeck A/S
20188553 66 Tetrahydroindolizinone NK1 antagonists.EBI Merck Research Laboratories
20560643 71 Improving metabolic stability by glycosylation: bifunctional peptide derivatives that are opioid receptor agonists and neurokinin 1 receptor antagonists.EBI University of Arizona
16562853 22 Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.EBI Tom's of Maine
18248994 16 Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.EBI Merck Research Laboratories
17407815 27 Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.EBI Johnson& Johnson Pharmaceutical Research& Development
16950620 36 N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.EBI Merck Sharp& Dohme Research Laboratories
16220969 219 Designed multiple ligands. An emerging drug discovery paradigm.EBI Organon Laboratories
15481976 17 Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.EBI Philipps-Universit£t Marburg
12190319 15 Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.EBI AstraZeneca Pharmaceuticals LP
11708932 7 An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.EBI Merck
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI F-59000 Lille
10691681 17 Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.EBI Clinical Research Institute of Montr£al
11052787 24 Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.EBI University of Pennsylvania
10090788 75 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).EBI SmithKline Beecham S.p.A.
10543877 25 Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides.EBI Uppsala University
9784098 8 Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements.EBI Takeda Chemical Industries, Ltd.
9703462 98 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.EBI Novartis Institute for Medical Sciences
8648606 72 Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.EBI Cambridge University Forvie Site
8691440 22 Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.EBI University of Pennsylvania
8691422 25 2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.EBI SmithKline Beecham S.p.A.
7699709 22 Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.EBI Merck Sharp& Dohme Research Laboratories
7515443 79 Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor.EBI Universit£ P. et M. Curie
8388471 28 Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs.EBI Institut de Recherches Servier
1370695 27 Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.EBI Rochester
1851847 22 Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists.EBI Rochester
2441057 22 Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.EBI TBA
11266174 51 Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.EBI Novartis Institute for Medical Sciences
11591520 6 Discovery of novel, orally active dual NK1/NK2 antagonists.EBI AstraZeneca Pharmaceuticals LP
9871670 13 Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.EBI Pfizer Inc.
9871768 7 Asymmetric synthesis of Boc-N-methyl-p-benzoyl-phenylalanine. Preparation of a photoreactive antagonist of substance P.EBI Universit£ P. et M. Curie
9871763 35 High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.EBI Merck Sharp Laboratory
 52 Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activityEBI TBA
 66 Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compoundsEBI TBA
 8 2,3-Substituted 2-azanorbornanes as polar -turn mimeticsEBI TBA
 22 The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonistsEBI TBA
 1 Synthesis of RPR 100893, prototype of a new series of potent and selective non peptide NK1 antagonists : the triarylperhydroisoindolols.EBI TBA
 24 The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug designEBI TBA
 31 An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.EBI TBA
22189275 26 Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.EBI Takeda Pharmaceutical Co. Ltd
21944973 31 Design, structure-activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor antagonists.EBI Takeda Pharmaceutical Co. Ltd
21937153 46 Recent progress in synthesis and bioactivity studies of indolizines.EBI University of Botswana
21925887 10 Synthesis and biological evaluation of new opioid agonist and neurokinin-1 antagonist bivalent ligands.EBI University of Arizona
21807525 30 3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.EBI Takeda Pharmaceutical Co. Ltd
21413804 21 Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.EBI Vrije Universiteit Brussel
21366266 66 Discovery of a potent and efficacious peptide derivative ford/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.EBI University of Arizona
21376585 120 Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.EBI Euroscreen SA
21292483 67 Identification of a new series of non-peptidic NK3 receptor antagonists.EBI H. Lundbeck A/S
21229983 19 Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.EBI GlaxoSmithKline Medicines Research Centre
20850972 11 Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.EBI F. Hoffmann-La Roche Ltd
20846861 20 Discovery of a series of potent, orally activea,a-disubstituted piperidine NK(1) antagonists.EBI Merck Research Laboratories
20729082 59 Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.EBI Merck Research Laboratories
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20617791 70 Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.EBI University of Arizona
20430616 36 Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.EBI F. Hoffmann-La Roche Ltd
20153964 44 Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.EBI Merck Research Laboratories
20178322 22 Discovery of dipeptides with high affinity to the specific binding site for substance P1-7.EBI Uppsala University
19963374 68 Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.EBI Pfizer Global Research and Development
19762245 69 The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.EBI University of Arizona
19817444 45 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.EBI F. Hoffmann-La Roche Ltd.
7517439 2 Spiroquinazoline, a Novel Substance P Inhibitor with a New Carbon Skeleton, Isolated from Aspergillus flavipesEBI TBA
7528269 2 1'-(2-Phenyl-ethylene)-ditryptophenaline, a New Dimeric Diketopiperazine from Aspergillus flavusEBI TBA
 9 Studies on the active conformation of the NK1 antagonist CGP 49823. Part 21. Fluoro-olefin analogs of tertiary amide rotamers.EBI TBA
 6 Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.EBI TBA
 14 3-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitutionEBI TBA
 10 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 vivoEBI TBA
 21 Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamidesEBI TBA
 10 1,4-Benzodiazepin-2-one derived neurokinin-1 receptor antagonistsEBI TBA
 11 Nonpeptide bradykinin antagonist analogs based on a model of a Sterling-Winthrop nonpeptide bradykinin antagonist overlapped with cyclic hexapeptide bradykinin antagonist peptidesEBI TBA
 41 Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptorsEBI TBA
 18 SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823EBI TBA
 8 The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptorsEBI TBA
 48 SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonistEBI TBA
 24 Linear amides as substance P antagonistsEBI TBA
 17 1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channelEBI TBA
 13 Structure-activity studies of the natural product substance P antagonist win 64821EBI TBA
 17 Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitutionEBI TBA
 15 Phenyl-glycinol based NK1 receptor antagonists — towards the minimum pharmacophoreEBI TBA
 4 Spiro-piperidine non-peptide neurokinin-1 receptor antagonistsEBI TBA
 17 4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonistsEBI TBA
 15 1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonistsEBI TBA
 12 Quinuclidine-based NK1 antagonists, the role of the benzhydrylEBI TBA
 6 N-alkyl quinuclidinium substance P antagonistsEBI TBA
 11 2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonistsEBI TBA
 4 Perhydrothiopyranopyrroles derivatives : A novel series of potent and selective nonpeptide NK1 antagonists.EBI TBA
 7 The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanesEBI TBA
 3 Gem-disubstituted amino-ether based substance p antagonistsEBI TBA
 6 Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirementsEBI TBA
 9 Acyclic NK1 antagonists: Replacements for the benzhydryl group.EBI TBA
 6 Morpholine-based substance P antagonists: assessment of the 3-point binding modelEBI TBA
 24 Acyclic NK-1 antagonists: 2-benzhydryl-2-aminoethyl ethersEBI TBA
 2 Articulating a pharmacophore driven synthetic strategy: Discovery of a potent substance P antagonistEBI TBA
 4 Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirementsEBI TBA
 17 Quinuclidine-based NK-1 antagonists I: 3-benzyloxy-1-azabicyclo[2.2.2]octanesEBI TBA
 5 Nuclear variations of quinuclidine substance P antagonists: 2-diphenylmethyl-1-azabicyclo[3.2.2]nonan-3-aminesEBI TBA
 6 Application of the multipin peptide synthesis technique for peptide receptor binding studies: Substance P as A model systemEBI TBA
 1 A facile synthesis of the novel Neurokinin A antagonist SR 48968EBI TBA
 20 1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.EBI TBA
 2 Conformationally restricted analogs of CP-99,994: synthesis of a spirocyclic amineEBI TBA
 1 Synthesis of RP-67,580, a new potent nonpeptide substance P antagonistEBI TBA
 5 Preparation and radiolabelling of CP-96,345, the first non-peptide substance P antagonistEBI TBA
19354254 24 Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.EBI Merck Research Laboratories
18829330 1 Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.EBI The University of Tokyo
18821747 45 The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.EBI University of Arizona
18640044 24 Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.EBI Pfizer Global Research & Development
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc.
18570365 29 The many roles for fluorine in medicinal chemistry.EBI Merck Research Laboratories
18554914 17 Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.EBI Università degli Studi di Siena
18547807 19 Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.EBI Schering-Plough Research Institute
18067242 6 Conformational comparisons of a series of tachykinin peptide analogs.EBI Mississippi State University
17967540 3 Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist.EBI Pfizer Global Research & Development
17919904 5 Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.EBI Pfizer Global Research & Development
17723300 55 Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.EBI Merck Research Laboratories
17637506 33 The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.EBI Merck & Co. Inc.
16950617 50 N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.EBI Merck Sharp & Dohme Research Laboratories
16884289 26 Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.EBI Merck Research Laboratories
16831551 31 Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.EBI Merck Research Laboratories
16824752 42 Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.EBI Merck Research Laboratories
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Global Research & Development
16698264 37 Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.EBI Merck Research Laboratories
16682196 19 Cyclobutane derivatives as potent NK1 selective antagonists.EBI Schering-Plough Research Institute
16580201 4 Diarylacetylene piperidinyl amides as novel anxiolytics.EBI Johnson & Johnson Pharmaceutical Research and Development LLC
16574413 28 NK1 antagonists based on seven membered lactam scaffolds.EBI Merck Sharp and Dohme Research Laboratories
16413782 20 1-Phenyl-8-azabicyclo[3.2.1]octane ethers: a novel series of neurokinin (NK1) antagonists.EBI Merck Sharp & Dohme Research Laboratories
16384700 24 Novel lactam NK1 antagonists with anti-emetic activity.EBI Merck Sharp & Dohme Research Laboratories
16332435 38 Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.EBI F. Hoffmann-La Roche Ltd
16307878 25 Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.EBI Merck Sharp & Dohme Research Laboratories
16290143 18 Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.EBI Schering-Plough Research Institute
16039119 35 Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.EBI Pfizer Global Research and Development
14998319 22 A non-peptide NK1 receptor agonist showing subpicomolar affinity.EBI Università degli Studi di Siena
14736234 11 Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.EBI AstraZeneca Pharmaceuticals LP
12723949 9 Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.EBI University of Pennsylvania
12372524 74 Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.EBI Schering-Plough Research Institute
12217362 10 Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.EBI Merck Sharp & Dohme Research Laboratories
12182850 19 Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.EBI Merck Sharp and Dohme Research Laboratories
12161132 102 Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.EBI Schering-Plough Research Institute
12127505 28 Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists.EBI Novartis Pharma AG
12067555 31 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.EBI Merck Sharp & Dohme Research Laboratories
12067554 27 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.EBI Merck Sharp & Dohme Research Laboratories
11859013 93 Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.EBI Schering-Plough Research Institute
11784148 81 Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI Pharmazeutisches Institut der Universität Freiburg
11755340 94 Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.EBI Schering-Plough Research Institute
11714615 22 Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides.EBI Novartis Pharma AG
11714604 19 2-Aryl indole NK(1) antagonists: optimisation of the amide substituent.EBI Merck Sharp & Dohme Research Laboratories
11428921 9 Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK(1) receptor antagonist.EBI Cambridge University Forvie Site
11425527 16 Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.EBI Lilly Research Laboratories
11354385 27 2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.EBI Merck, Sharp and Dohme Research Laboratories
11354384 27 2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.EBI The Neuroscience Research Centre
11266164 3 Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.EBI Laboratoire de Chimie Thérapeutique associé au CNRS et à l'Université René Descartes (UMR 8638)
11229755 66 Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.EBI Schering-Plough Research Institute
11087566 69 Multiple-conformation and protonation-state representation in 4D-QSAR: the neurokinin-1 receptor system.EBI Biographics Laboratory 3R
11055350 58 Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.EBI Schering-Plough Research Institute
11055349 19 The design and synthesis of novel NK1/NK2 dual antagonists.EBI Schering-Plough Research Institute
10888334 10 N-[(R,R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3,5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist.EBI Novartis Pharma AG
10794691 8 Solution structures in SDS micelles and functional activity at the bullfrog substance P receptor of ranatachykinin peptides.EBI Marshall University School of Medicine and Huntington VA Medical Center
10737756 1 Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.EBI Merck Research Laboratories
10508446 12 Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.EBI Takeda Chemical Industries, Ltd.
9873524 37 L-tryptophan urea amides as NK1/NK2 dual antagonists.EBI Merck Research Laboratories
9873446 12 Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.EBI Merck Sharp and Dohme Research Laboratories
9873445 41 Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.EBI Merck Sharp and Dohme Research Laboratories
9871627 20 High affinity phenylglycinol-based NK1 receptor antagonists.EBI Merck Sharp and Dohme Research Laboratories
9804702 37 4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.EBI Merck, Sharp and Dohme Research Laboratories
9804700 10 Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.EBI Merck Research Laboratories
9554871 43 Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.EBI University of Pennsylvania
9191956 51 Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.EBI SmithKline Beecham S.p.A. Milano
8709125 11 N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.EBI Merck Sharp and Dohme Research Laboratories
8627597 17 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.EBI Merck Research Laboratories
8576917 79 3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.EBI Lilly Research Laboratories
8393115 11 N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.EBI Merck, Sharp and Dohme Research Laboratories
7731011 5 4,4-Disubstituted piperidines: a new class of NK1 antagonist.EBI Merck, Sharp and Dohme Research Laboratories
7543579 46 Novel, potent, and orally active substance P antagonists: synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine.EBI Takeda Chemical Industries, Ltd.
7535362 39 Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.EBI Merck, Sharp & Dohme Research Laboratories
7527861 3 Importance of parallel vectors and"hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist.EBI Pfizer Inc.
7520943 16 Aza-tricyclic substance P antagonists.EBI Pfizer, Inc.
7518522 12 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.EBI Technische Universität München
7513763 92 Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.EBI Merck, Sharp and Dohme Research Laboratories
7508512 21 Structure determination, pharmacological evaluation, and structure-activity studies of a new cyclic peptide substance P antagonist containing the new amino acid 3-prenyl-beta-hydroxytyrosine, isolated from Aspergillus flavipes.EBI Sterling Winthrop Pharmaceuticals Research Division
7490729 62 Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.EBI Merck, Sharp and Dohme Research Laboratories
2433443 9 Antagonists of substance P. Further modifications of substance P antagonists obtained by replacing either positions 7, 9 or 7, 8 and 11 of SP with D-amino acid residues.EBI TBA
1378901 18 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.EBI Pfizer, Inc.
1373191 15 Synthesis and substance P antagonist activity of naphthimidazolium derivatives.EBI Rochester
1282570 6 Discovery of a potent substance P antagonist: recognition of the key molecular determinant.EBI Pfizer Inc.
15831442 46 Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.BDB Taisho Pharmaceutical Co., Ltd
15131245 86 SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.BDB Sanofi-Synthelabo Recherche
12721338 61 N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.BDB Pudue Pharma Discovery Research
12438541 27 SSR240600 [(R)-2-(1-[2-[4-[2-[3,5-bis(trifluoromethyl)phenyl]acetyl]-2-(3,4-dichlorophenyl)-2-morpholinyl]ethyl]- 4-piperidinyl)-2-methylpropanamide], a centrally active nonpeptide antagonist of the tachykinin neurokinin-1 receptor: I. biochemical and pharmacological characterization.BDB Sanofi-Synthélabo Recherche
12431845 84 Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder.BDB Lilly Research Laboratories
12206858 11 SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist.BDB Schering-Plough Research Institute
11750183 29 Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.BDB Novartis Pharma
11750180 139 Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.BDB Lilly Research Laboratories
11438309 51 The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.BDB Janssen Research Foundation
11408556 2 Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors.BDB AstraZeneca Pharmaceuticals
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
9454810 72 SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.BDB Sanofi Recherche
9225287 174 RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.BDB Roche Bioscience
9190866 26 Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.BDB SmithKline Beecham Pharmaceuticals
8887981 72 A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.BDB Abbott Laboratories
8627566 53 In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist.BDB Hoechst Marion Roussel
8012715 38 GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.BDB Glaxo Group Research Ltd.
7830490 21 SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.BDB Sanofi Recherche
7518514 46 (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.BDB Abbott Laboratories
17516639 29 Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.BDB University of Arizona at Tucson
18266313 30 A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists.BDB University of Arizona at Tucson