The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27997171 |
48 |
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. |
The University of Newcastle |
| 28523109 |
79 |
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. |
Glaxosmithkline |
| 27876250 |
60 |
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 |
| 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. |
Jagiellonian University Medical College |
| 26005524 |
147 |
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. |
Merck Research Laboratories |
| 25738882 |
210 |
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I). |
Euroscreen |
| 24983484 |
11 |
Toward fluorescent probes for G-protein-coupled receptors (GPCRs). |
Shandong University |
| 17604625 |
63 |
alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists. |
Menarini Ricerche |
| 24175572 |
1 |
6-Alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds. |
F. Hoffmann-La Roche |
| 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. |
Merck Research Laboratories |
| 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. |
Institute of Organic Synthesis |
| 23466604 |
36 |
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
Universit£ |
| 23477943 |
51 |
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression. |
Bristol-Myers Squibb |
| 21320781 |
9 |
hNK2 receptor antagonists. The use of intramolecular hydrogen bonding to increase solubility and membrane permeability. |
Menarini Ricerche |
| 20408549 |
50 |
Structure-activity relationships of 6-methyl-benzo[b]thiophene-2-carboxylic acid (1-[(S)-1-benzyl-4-[4-(tetrahydropyran-4-ylmethyl)piperazin-1-yl]butylcarbamoyl]cyclopentyl)amide, potent antagonist of the neurokinin-2 receptor. |
Menarini Ricerche |
| 18640835 |
1 |
Cinnamic acids and mono-substituted benzoic acids as useful capping groups for the preparation of hNK2 receptor antagonists. |
Menarini Ricerche |
| 11844703 |
14 |
Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor. |
Menarini Ricerche S.P.A. Laboratori Di Firenze |
| 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. |
F. Hoffmann-La Roche |
| 20931963 |
112 |
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 |
| 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. |
H. Lundbeck |
| 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. |
Tom'S of Maine |
| 16950620 |
36 |
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists. |
Merck Sharp & Dohme Research Laboratories |
| 16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
| 12190319 |
15 |
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity. |
Astrazeneca Pharmaceuticals |
| 11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
| 11052787 |
24 |
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry. |
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). |
Smithkline Beecham |
| 10425111 |
17 |
Importance of the aromatic residue at position 6 of [Nle(10)]neurokinin A(4-10) for binding to the NK-2 receptor and receptor activation. |
Creighton University School of Medicine |
| 8691422 |
25 |
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. |
Smithkline Beecham |
| 8388471 |
28 |
Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs. |
Institut De Recherches Servier |
| 11591520 |
6 |
Discovery of novel, orally active dual NK1/NK2 antagonists. |
Astrazeneca Pharmaceuticals |
| 9871763 |
35 |
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template. |
Merck Sharp Laboratory |
| | 3 |
Two novel amino acid derivatives containing side-chain thioamides for the synthesis of photoactivatable peptides |
TBA |
| | 52 |
Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity |
TBA |
| 21937153 |
46 |
Recent progress in synthesis and bioactivity studies of indolizines. |
University of Botswana |
| 21376585 |
120 |
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor. |
Euroscreen |
| 21292483 |
67 |
Identification of a new series of non-peptidic NK3 receptor antagonists. |
H. Lundbeck |
| 20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
| 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. |
F. Hoffmann-La Roche |
| | 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 vivo |
TBA |
| | 41 |
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors |
TBA |
| | 2 |
A Non-peptidic photoactivatable antagonist for mapping the antagonist binding site of the tachykinin NK2 receptor |
TBA |
| | 17 |
Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution |
TBA |
| | 24 |
Substituted 2,4-diaminoquinazolines and 2,4-diamino-8-alkylpurines as antagonists of the neurokinin-2 (NK2) receptor |
TBA |
| 19354254 |
24 |
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. |
Merck Research Laboratories |
| 19271735 |
35 |
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). |
Wyeth Research |
| 18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
| 17428923 |
38 |
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe. |
Pharmaceutical Research Institute |
| 17637506 |
33 |
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine. |
Merck |
| 16950617 |
50 |
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II. |
Merck Sharp & Dohme Research Laboratories |
| 16876401 |
48 |
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. |
Jerini |
| 16698264 |
37 |
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists. |
Merck Research Laboratories |
| 16580201 |
4 |
Diarylacetylene piperidinyl amides as novel anxiolytics. |
Johnson & Johnson Pharmaceutical Research and Development |
| 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. |
Pfizer |
| 15664817 |
86 |
Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'. |
Menarini Ricerche |
| 14736234 |
11 |
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties. |
Astrazeneca Pharmaceuticals |
| 12798336 |
21 |
4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor. |
Pfizer |
| 12372524 |
74 |
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines. |
Schering-Plough Research Institute |
| 12161132 |
102 |
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity. |
Schering-Plough Research Institute |
| 12161112 |
14 |
Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor. |
Universita' Di Firenze |
| 12127505 |
28 |
Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists. |
Novartis Pharma |
| 11859013 |
93 |
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications. |
Schering-Plough Research Institute |
| 11784148 |
81 |
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1. |
Pharmazeutisches Institut Der UniversitäT Freiburg |
| 11755340 |
94 |
Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides. |
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. |
Novartis Pharma |
| 11356103 |
61 |
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists. |
Smithkline Beecham Pharmaceuticals |
| 11277528 |
7 |
Spatial requirements of the antagonist binding site of the NK2 receptor. |
University of Leeds |
| 11229755 |
66 |
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors. |
Schering-Plough Research Institute |
| 11055350 |
58 |
Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines. |
Schering-Plough Research Institute |
| 11055349 |
19 |
The design and synthesis of novel NK1/NK2 dual antagonists. |
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. |
Novartis Pharma |
| 31112891 |
30 |
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity. |
National University of Ireland Galway |
| 9873524 |
37 |
L-tryptophan urea amides as NK1/NK2 dual antagonists. |
Merck Research Laboratories |
| 9873462 |
19 |
4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor. |
Zeneca Pharmaceuticals |
| 9871627 |
20 |
High affinity phenylglycinol-based NK1 receptor antagonists. |
Merck Sharp and Dohme Research Laboratories |
| 30964988 |
26 |
Design and Identification of a Novel, Functionally Subtype Selective GABA |
Pfizer |
| 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. |
Smithkline Beecham S.P.A. Milano |
| 31082225 |
26 |
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms. |
China Pharmaceutical University |
| 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. |
Merck Research Laboratories |
| 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. |
Technische UniversitäT MüNchen |
| 7513763 |
92 |
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. |
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. |
Sterling Winthrop Pharmaceuticals Research Division |
| 17850056 |
58 |
Discovery of a new series of potent and selective linear tachykinin NK2 receptor antagonists. |
Menarini Ricerche |
| 15615542 |
52 |
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 |
| 12139452 |
29 |
Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies. |
Menarini Ricerche |
| 11063600 |
32 |
Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists. |
Menarini Ricerche |
| 7562907 |
33 |
New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists. |
Glaxo Wellcome Medicines Research Centre |
| 8027981 |
8 |
Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor. |
Glaxo Institute For Molecular Biology |
| 30015488 |
44 |
Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium. |
University of Florida |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 23031230 |
5 |
Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases. |
Universit?? Degli Studi Di Siena |
| 23792961 |
10 |
Site-specific inhibitory mechanism for amyloid ß42 aggregation by catechol-type flavonoids targeting the Lys residues. |
Kyoto University |
| 26833890 |
18 |
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. |
Yogi Vemana University |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
| 9808667 |
12 |
Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides. |
Dupont Pharmaceuticals |
| 8821530 |
16 |
In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. |
Smithkline Beecham Pharmaceuticals |
| 17064063 |
18 |
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Abbott Laboratories |
| 10891109 |
19 |
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2. |
Palacky University |
Search and Browse
