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74 articles for thisTarget


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

PMID
Data
Article Title
Organization
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.EBI
Merck Sharp and Dohme Research Laboratories
Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)-oxazoles).EBI
Merck Sharp and Dohme Research Laboratories
Novel 5-HT3 antagonists. Indole oxadiazoles.EBI
Merck Sharp and Dohme Research Laboratories
Spiropiperidines as high-affinity, selective sigma ligands.EBI
Merck Sharp and Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.EBI
Merck Sharp and Dohme Research Laboratories
Cyclic peptides as selective tachykinin antagonists.EBI
Merck Sharp and Dohme Research Laboratories
2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.EBI
Merck Sharp and Dohme Research Laboratories
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
Current and novel approaches to the drug treatment of schizophrenia.EBI
Merck Sharp and Dohme Research Laboratories
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.EBI
Merck Sharp and Dohme Research Laboratories
HIV protease: a novel chemotherapeutic target for AIDS.EBI
Merck Sharp and Dohme Research Laboratories
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.EBI
Merck Sharp and Dohme Research Laboratories
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.EBI
Merck Sharp and Dohme Research Laboratories
Phosphinic acid inhibitors of D-alanyl-D-alanine ligase.EBI
Merck Sharp and Dohme Research Laboratories
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.EBI
Merck Sharp and Dohme Research Laboratories
3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.EBI
Merck Sharp and Dohme Research Laboratories
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.EBI
Merck Sharp and Dohme Research Laboratories
NK1 antagonists based on seven membered lactam scaffolds.EBI
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.EBI
Merck Sharp and Dohme Research Laboratories
8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.EBI
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp and Dohme Research Laboratories
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.EBI
Merck Sharp and Dohme Research Laboratories
Sarcosine based indandione hGlyT1 inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.EBI
Merck Sharp and Dohme Research Laboratories
Cyclic sulfamide gamma-secretase inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.EBI
Merck Sharp and Dohme Research Laboratories
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.EBI
Merck Sharp and Dohme Research Laboratories
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.EBI
Merck Sharp and Dohme Research Laboratories
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.EBI
Merck Sharp and Dohme Research Laboratories
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.EBI
Merck Sharp and Dohme Research Laboratories
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.EBI
Merck Sharp and Dohme Research Laboratories
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.EBI
Merck Sharp and Dohme Research Laboratories
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.EBI
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.EBI
Merck Sharp and Dohme Research Laboratories
Serine derived NK1 antagonists. 1: The effect of modifications to the serine substituents.EBI
Merck Sharp and Dohme Research Laboratories
High affinity phenylglycinol-based NK1 receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
4,4-Disubstituted piperidine high-affinity NK1 antagonists: structure-activity relationships and in vivo activity.EBI
Merck Sharp and Dohme Research Laboratories
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.EBI
Merck Sharp and Dohme Research Laboratories
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.EBI
Merck Sharp and Dohme Research Laboratories
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.EBI
Merck Sharp and Dohme Research Laboratories
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.EBI
Merck Sharp and Dohme Research Laboratories
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.EBI
Merck Sharp and Dohme Research Laboratories
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.EBI
Merck Sharp and Dohme Research Laboratories
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.EBI
Merck Sharp and Dohme Research Laboratories
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.EBI
Merck Sharp and Dohme Research Laboratories
N-acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists.EBI
Merck Sharp and Dohme Research Laboratories
3-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors.EBI
Merck Sharp and Dohme Research Laboratories
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.EBI
Merck Sharp and Dohme Research Laboratories
Identification of 3,5-dihydro-2-aryl-1H-pyrazolo[3,4-c]quinoline-1,4(2H)-diones as novel high-affinity glycine site N-methyl-D-aspartate antagonists.EBI
Merck Sharp and Dohme Research Laboratories
4,4-Disubstituted piperidines: a new class of NK1 antagonist.EBI
Merck Sharp and Dohme Research Laboratories
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor.EBI
Merck Sharp and Dohme Research Laboratories
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.EBI
Merck Sharp and Dohme Research Laboratories
Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.EBI
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.EBI
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.EBI
Merck Sharp and Dohme Research Laboratories
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.EBI
Merck Sharp and Dohme Research Laboratories
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.EBI
Merck Sharp and Dohme Research Laboratories
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.EBI
Merck Sharp and Dohme Research Laboratories
Isoquinolin-3-yl carboxamides and preparation and use thereofBDB
Samumed
Cyclosporin analogues for preventing or treating hepatitis C infectionBDB
Enanta Pharmaceuticals
Compositions useful for treating disorders related to kitBDB
Blueprint Medicines
Opioid agonists and uses thereofBDB
Nektar Therapeutics
Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance.BDB
Purdue University
Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.BDB
Banyu Pharmaceutical