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92 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review

Article Title
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.EBI
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
Development of novel NK3 receptor antagonists with reduced environmental impact.EBI
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.EBI
Jagiellonian University Medical College
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).EBI
Euroscreen SA
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).EBI
Euroscreen SA
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation.EBI
Kyoto University
Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.EBI
Universit£ de Montr£al
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.EBI
Universit£ de Montr£al
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
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
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.EBI
Universit£ degli Studi di Siena
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 Co.
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.EBI
Kyoto University
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor.EBI
Northeast Ohio Medical University
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia.EBI
New quinoline NK3 receptor antagonists with CNS activity.EBI
Neuroscience CEDD GlaxoSmithKline Research & Development
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 Inc
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.EBI
ASKA Pharmaceutical Co., Ltd
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.EBI
Merck Sharp & Dohme Research Laboratories
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.EBI
AstraZeneca Pharmaceuticals LP
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.
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists.EBI
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.EBI
SmithKline Beecham S.p.A.
Discovery of novel, orally active dual NK1/NK2 antagonists.EBI
AstraZeneca Pharmaceuticals LP
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.EBI
Merck Sharp Laboratory
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compoundsEBI
2,3-Substituted 2-azanorbornanes as polar -turn mimeticsEBI
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonistsEBI
The design of polar -turn dipeptide mimeticsEBI
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug designEBI
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.EBI
Euroscreen SA
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists.EBI
AstraZeneca Pharmaceuticals
Identification of a new series of non-peptidic NK3 receptor antagonists.EBI
H. Lundbeck A/S
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor.EBI
Northeastern Ohio Universities Colleges of Medicine and Pharmacy
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.EBI
F. Hoffmann-La Roche Inc
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI
Università degli Studi di Milano
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands.EBI
F. Hoffmann-La Roche Inc
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 Inc
A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonistEBI
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonistEBI
Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitutionEBI
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanesEBI
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening.EBI
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.EBI
Merck Research Laboratories
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.EBI
Schering-Plough Research Institute
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.EBI
Merck & Co. Inc
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.EBI
Merck Sharp & Dohme Research Laboratories
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.EBI
Merck Research Laboratories
Cyclobutane derivatives as potent NK1 selective antagonists.EBI
Schering-Plough Research Institute
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.EBI
AstraZeneca Pharmaceuticals LP
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity.EBI
Schering-Plough Research Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI
Pharmazeutisches Institut der Universität Freiburg
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.EBI
SmithKline Beecham Pharmaceuticals Ltd
Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact.EBI
Kyoto University
High affinity phenylglycinol-based NK1 receptor antagonists.EBI
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.EBI
SmithKline Beecham S.p.A. Milano
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.EBI
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.EBI
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.EBI
Technische Universität München
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.EBI
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.EBI
Menarini Ricerche S.p.A.
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI
Phenex Pharmaceuticals AG
Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.BDB
UniversitÓ degli Studi di Siena
Defining the communication between agonist and coactivator binding in the retinoid X receptor a ligand binding domain.BDB
University of Alabama at Birmingham
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.BDB
Yogi Vemana University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides.BDB
DuPont Pharmaceuticals Company
In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.BDB
SmithKline Beecham Pharmaceuticals Ltd
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.BDB
Abbott Laboratories
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2.BDB
Palacky University