PMID

Data

Article Title

Organization

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.

The University of Newcastle

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

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

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.

Merck Research Laboratories

Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).

Euroscreen

Toward fluorescent probes for G-protein-coupled receptors (GPCRs).

Shandong University

alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists.

Menarini Ricerche

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

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.

Universit£

Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.

Bristol-Myers Squibb

hNK2 receptor antagonists. The use of intramolecular hydrogen bonding to increase solubility and membrane permeability.

Menarini Ricerche

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

Cinnamic acids and mono-substituted benzoic acids as useful capping groups for the preparation of hNK2 receptor antagonists.

Menarini Ricerche

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

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

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

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

N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.

Merck Sharp & Dohme Research Laboratories

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.

Astrazeneca Pharmaceuticals

From hit to lead. Analyzing structure-profile relationships.

Universities of Lille

Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.

University of Pennsylvania

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

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

2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.

Smithkline Beecham

Tetrapeptide tachykinin antagonists: synthesis and modulation of the physicochemical and pharmacological properties of a new series of partially cyclic analogs.

Institut De Recherches Servier

Discovery of novel, orally active dual NK1/NK2 antagonists.

Astrazeneca Pharmaceuticals

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.

Merck Sharp Laboratory

 

Two novel amino acid derivatives containing side-chain thioamides for the synthesis of photoactivatable peptides

TBA

 

Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity

TBA

Recent progress in synthesis and bioactivity studies of indolizines.

University of Botswana

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.

Euroscreen

Identification of a new series of non-peptidic NK3 receptor antagonists.

H. Lundbeck

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Università

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

 

A Non-peptidic photoactivatable antagonist for mapping the antagonist binding site of the tachykinin NK₂ receptor

TBA

 

Piperidine-ether based hNK₁ antagonists 2: Investigation of the effect of N-substitution

TBA

 

Substituted 2,4-diaminoquinazolines and 2,4-diamino-8-alkylpurines as antagonists of the neurokinin-2 (NK₂) receptor

TBA

Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.

Merck Research Laboratories

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

Highly functionalized 7-azaindoles as selective PPAR gamma modulators.

Merck Research Laboratories

Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.

Pharmaceutical Research Institute

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

Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity.

Jerini

Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.

Merck Research Laboratories

Diarylacetylene piperidinyl amides as novel anxiolytics.

Johnson & Johnson Pharmaceutical Research and Development

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

Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'.

Menarini Ricerche

JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.

Janssen Research & Development

Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.

Astrazeneca Pharmaceuticals

4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor.

Pfizer

Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.

Schering-Plough Research Institute

Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.

Schering-Plough Research Institute

Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor.

Universita' Di Firenze

Biphenyl derivatives as novel dual NK(1)/NK(2)-receptor antagonists.

Novartis Pharma

Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.

Schering-Plough Research Institute

Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.

Pharmazeutisches Institut Der UniversitäT Freiburg

Synthesis and structure-activity relationships of oxime neurokinin antagonists: discovery of potent arylamides.

Schering-Plough Research Institute

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

Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.

Smithkline Beecham Pharmaceuticals

Spatial requirements of the antagonist binding site of the NK2 receptor.

University of Leeds

Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.

Schering-Plough Research Institute

Synthesis and NK1/NK2 receptor activity of substituted-4(Z)-(methoxyimino)pentyl-1-piperazines.

Schering-Plough Research Institute

The design and synthesis of novel NK1/NK2 dual antagonists.

Schering-Plough Research Institute

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

Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.

National University of Ireland Galway

L-tryptophan urea amides as NK1/NK2 dual antagonists.

Merck Research Laboratories

4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor.

Zeneca Pharmaceuticals

High affinity phenylglycinol-based NK1 receptor antagonists.

Merck Sharp and Dohme Research Laboratories

Design and Identification of a Novel, Functionally Subtype Selective GABA

Pfizer

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

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

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

Discovery of a new series of potent and selective linear tachykinin NK2 receptor antagonists.

Menarini Ricerche

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

Monocyclic human tachykinin NK-2 receptor antagonists as evolution of a potent bicyclic antagonist: QSAR and site-directed mutagenesis studies.

Menarini Ricerche

Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.

Menarini Ricerche

New spiropiperidines as potent and selective non-peptide tachykinin NK2 receptor antagonists.

Glaxo Wellcome Medicines Research Centre

Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor.

Glaxo Institute For Molecular Biology

Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium.

University of Florida

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.

Universit?? Degli Studi Di Siena

Site-specific inhibitory mechanism for amyloid ß42 aggregation by catechol-type flavonoids targeting the Lys residues.

Kyoto 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.

Yogi Vemana University

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University of Leipzig

Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides.

Dupont Pharmaceuticals

In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.

Smithkline Beecham Pharmaceuticals

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

Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.

Palacky University