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

Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.

Sankyo

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.

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

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

Cyclic peptides as selective tachykinin antagonists.

Merck Sharp and Dohme Research Laboratories

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

Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration.

Umr Uds/Cnrs 7200

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 and synthesis of substituted N-methylbenzamide analogues derived from SR 48,968 as neurokinin-2 receptor antagonists.

St. John'S University

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

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

Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.

Pfizer

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

Institut De Recherches Servier

Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.

Glaxo Group Research

A new class of high affinity ligands for the neurokinin A NK2 receptor: psi (CH2NR) reduced peptide bond analogues of neurokinin A4-10.

Marion Merrell Dow Research Institute

Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists.

Rochester

Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.

The Schering Plough Research Institute

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

 

Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds

TBA

 

2,3-Substituted 2-azanorbornanes as polar -turn mimetics

TBA

 

The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists

TBA

 

The design of polar -turn dipeptide mimetics

TBA

 

The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design

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

Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.

University of Arizona

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

 

Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK₁/NK₂ receptor antagonists

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

 

SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK₁ antagonist

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

 

Alternative strategies towards the identification of chemical lead compounds by rational design

TBA

 

Methionine replacements in biologically active peptides

TBA

 

Pharmacological profile and chemical synthesis of SR 48968, a non-peptide antagonist of the neurokinin A (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

Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.

Sankyo

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

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

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 RORγt.

Phenex Pharmaceuticals

Potent and highly selective neurokinin antagonists.

Glaxo Group Research

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

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

Hoffmann-La Roche

Azalactam compounds as HPK1 inhibitors

Pfizer

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

PDE4 inhibitor

Shijiazhuang Sagacity New Drug Development

Heterocyclic compounds as inhibitors of platelet aggregation

Universite De Montreal

Heterocyclic inhibitors of monocarboxylate transporter

The Scripps Research Institute

Pyrrolotriazine inhibitors of IRAK4 activity

Merck Sharp & Dohme

Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

Ctxt

Methods of use of cyclopamine analogs

Infinity Pharmaceuticals

Therapeutic compounds and uses thereof

Genentech

8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives

Idorsia Pharmaceuticals

Compounds as rearranged during transfection (RET) inhibitors

Glaxosmithkline

Heterocyclic kinase inhibitors

Abbvie

Complement pathway modulators and uses thereof

Novartis

Ocular formulations for drug-delivery to the posterior segment of the eye

Panoptica

Human UTY(KDM6C) is a male-specific N¿-methyl lysyl demethylase.

University of Oxford

Hepatitis C virus inhibitors

Bristol-Myers Squibb

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

Tetrahydrothiazepine derivative

Daiichi Sankyo

Isoxazolo-pyridine derivatives

Roche Palo Alto

Splicing factor SF3b as a target of the antitumor natural product pladienolide.

Eisai

Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.

Griffith University

Biarylether amide quinolines as liver X receptor agonists.

Wyeth Research

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

Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases.

Medical University of South Carolina