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140 articles for thisTarget

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

Article Title
Studies on quinazolines. 5. 2,3-dihydroimidazo[1,2-c]quinazoline derivatives: a novel class of potent and selective alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
National Defense Medical Center
2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents.EBI
R. W. Johnson Pharmaceutical Research Institute
Structure-affinity relationships of 12-sulfonyl derivatives of 5,8,8a,9,10,11,12,12a,13,13a-decahydro-6H-isoquino[2,1-g][1 ,6] naphthyridines at alpha-adrenoceptors.EBI
Syntex Research
1,9-Alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines with affinity for the alpha 2-adrenoceptor and the 5-HT1A receptor.EBI
Syntex Research
Affinity of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha 2-adrenoceptor vs the [3H]yohimbine-labeled site.EBI
Syntex Research
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.EBI
Syntex Research
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.EBI
Reckitt & Colman plc
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.EBI
Institut de Pharmacologie (UA 589 CNRS)
Structure-activity relationships among benextramine-related tetraamine disulfides. Chain length effect on alpha-adrenoreceptor blocking activity.EBI
University of Camerino
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.EBI
Reckitt and Colman plc
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists.EBI
Pfizer Inc
2,4-Diamino-6,7-dimethoxyquinoline derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
Pfizer Inc
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
Pfizer Inc
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.EBI
Synthesis and antidepressant properties of novel 2-substituted 4,5-dihydro-1H-imidazole derivatives.EBI
2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.EBI
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
Pfizer Inc
2,4-diamino-6,7-dimethoxyquinazolines. 1. 2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.EBI
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.EBI
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.EBI
Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.EBI
Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.EBI
6,7-Dihydro-5-[[(cis-2-hydroxy-trans-3-phenoxycyclopentyl)amino] methyl]-2-methylbenzo[b]thiophen-4(5H)-one: a novel alpha 1-adrenergic receptor antagonist and renal vasodilator.EBI
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.EBI
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.EBI
Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.EBI
Conformationally defined adrenergic agents. 1. Design and synthesis of novel alpha 2 selective adrenergic agents: electrostatic repulsion based conformational prototypes.EBI
Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.EBI
Antihypertensive 9-substituted 1-oxa-4,9-diazaspiro[5.5]undecan-3-ones.EBI
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.EBI
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.EBI
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.EBI
Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines.EBI
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines.EBI
Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists.EBI
Pfizer Inc
alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds.EBI
Universit£ di Pisa
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.EBI
University of Kansas
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.EBI
Universidade Federal de Goi£s
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.EBI
Merrell Dow Research Institute
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.EBI
University of Bologna
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.EBI
European Research Centre for Drug Discovery and Development (NatSynDrugs)
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.EBI
Universit£ degli Studi di Urbino Carlo Bo
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.EBI
Universit£ di Siena
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.EBI
Abbott Laboratories
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).EBI
Hoechst-Roussel Pharmaceuticals Inc
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.EBI
SmithKline Beecham Pharmaceuticals Ltd
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).EBI
Abbott Laboratories
The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.EBI
Sandoz Pharma Limited
Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.EBI
National Institute of Diabetes and Digestive and Kidney Diseases
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.EBI
University of Pennsylvania
Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives.EBI
Universit£ di Pisa
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.EBI
Searle Research and Development
Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.EBI
Universit£ di Pisa
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.EBI
Bristol-Myers Squibb Co.
Novel benzamides as selective and potent gastrokinetic agents. 2. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2- morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds.EBI
Dainippon Pharmaceutical Company, Ltd.
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.EBI
Warner-Lambert Company
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.EBI
Pfizer Inc
The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity.EBI
Bristol-Myers Company
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.EBI
Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents.EBI
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.EBI
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.EBI
Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents.EBI
Universit£ degli Studi di Siena
Novel pyridazino[4,5-b][1,5]oxazepines and -thiazepines as 5-HT1A receptor ligandsEBI
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamidesEBI
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.EBI
European Research Centre for Drug Discovery and Development (NatSynDrugs)
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.EBI
Dipartimento di Scienze Farmaceutiche
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.EBI
Predix Pharmaceuticals Ltd.
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.EBI
University of Kansas
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.EBI
Virginia Commonwealth University
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.EBI
Virginia Commonwealth University
Binding of an imidazopyridoindole at imidazoline I2 receptors.EBI
Virginia Commonwealth University
1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.EBI
F. Hoffmann-La Roche Inc
Development of a presynaptic 5-HT1A antagonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus.EBI
Università di Pisa
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine EBI
University of Kansas
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.EBI
University of Crete
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI
The R. W. Johnson Pharmaceutical Research Institute
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.EBI
Università di Perugia
Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.EBI
University of Bristol
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.EBI
The R. W. Johnson Pharmaceutical Research Institute
Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.EBI
Warner-Lambert Company
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.EBI
Knoll Pharmaceuticals
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.EBI
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).EBI
Centro de Investigación Grupo Ferrer
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.EBI
Parke-Davis Pharmaceutical Research
Serotonergic ergoline derivatives.EBI
Pharmacia & Upjohn
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.EBI
Warner-Lambert Company
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.EBI
Hoechst-Roussel Pharmaceuticals Inc
(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors.EBI
Wyeth Research (UK)
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.EBI
Mayo Foundation
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly and Company
Fluorinated analogues of marsanidine, a highly ?2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities.EBI
Medical University of Gdansk
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.EBI
Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines.EBI
Absolute configuration of glycerol derivatives. 4. Synthesis and pharmacological activity of chiral 2-alkylaminomethylbenzodioxans, competitive alpha-adrenergic antagonists.EBI
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar B.V.
Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.EBI
Universidade Federal do Rio de Janeiro
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone.EBI
Jagiellonian University Medical College
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.EBI
Universit£ degli Studi di Camerino
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.EBI
Rzesz£w University of Technology
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.EBI
Solvay Pharma
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.EBI
Universit£ degli Studi di Camerino
Alpha2-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole.EBI
Universit£ degli Studi di Camerino
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.EBI
Institut de Recherches Servier
Synthesis and biological properties of thiophene ring analogues of mianserin.EBI
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.EBI
Universit£ di Perugia
Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles.EBI
The R. W. Johnson Pharmaceutical Research Institute
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.EBI
University of Bologna
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.EBI
University of Camerino
2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.EBI
Universit£ di Camerino
Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket".EBI
University of Tennessee
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.EBI
Monash University
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.EBI
University of Camerino
Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.EBI
Ohio State University
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI
Huazhong University of Science and Technology
In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.EBI
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system.EBI
Jagiellonian University Medical College
N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.EBI
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.EBI
Warner-Lambert Company
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.EBI
Dipartimento di Farmacia Universit£ di Napoli "Federico II" Via D. Montesano
Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HTEBI
Jagiellonian University Medical College
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI
Phenex Pharmaceuticals AG
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.EBI
University of California
Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.EBI
Abbott Laboratories
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.BDB
University of Karachi