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BindingDB contains 2.6M data for 1.1M Compounds and 8.9K Targets. Of those, 1,167K data for 538K Compounds and 4.4K Targets were curated by BindingDB curators.

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452 articles for thisTarget


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PMID
Data
Article Title
Organization
Synthetic Approaches to the New Drugs Approved During 2015.EBI
Pfizer Inc
Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine DEBI
National Institute on Drug Abuse-Intramural Research Program
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.EBI
Friedrich-Alexander University Erlangen-N£rnberg
Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase.EBI
Universit£ di Bologna
Asymmetric total synthesis of tetrahydroprotoberberine derivatives and evaluation of their binding affinities at dopamine receptors.EBI
Harvard Medical School
4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone: a prejunctional dopamine receptor agonist.EBI
TBA
4-(Aminoalkyl)-7-hydroxy-2(3H)-indolones, a novel class of potent presynaptic dopamine receptor agonists.EBI
TBA
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.EBI
GlaxoSmithKline
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.EBI
GlaxoSmithKline
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.EBI
Centre de Recherches de Croissy
Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.EBI
SmithKline Beecham Pharmaceuticals Ltd
Synthesis and evaluation of C9 alkoxy analogues of (-)-stepholidine as dopamine receptor ligands.EBI
City University of New York
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
Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.EBI
Shanghai Jiao Tong University
Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5-HTEBI
Universit£ de Montr£al
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University of Kansas
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.EBI
National Institute on Drug Abuse
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.EBI
Florida A&M University
1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.EBI
Aptuit s.r.l
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.EBI
Florida A&M University
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.EBI
Florida A&M University
Structure-guided development of dual▀2 adrenergic/dopamine D2 receptor agonists.EBI
Friedrich-Alexander University
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.EBI
Columbia University College of Physicians and Surgeons
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.EBI
Abbott Healthcare Products BV
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.EBI
Vanderbilt 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
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.EBI
Aptuit s.r.l
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity.EBI
City University of New York
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.EBI
University of Illinois at Chicago
Improving selectivity of dopamine D3 receptor ligands.EBI
Bioprojet-Biotech
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.EBI
The Alexander Shulgin Research Institute
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI
Aptuit s.r.l
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.EBI
Huazhong University of Science and Technology
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI
City University of New York
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.EBI
Glenmark Research Centre
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.EBI
Universit degli Studi di Milano
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.EBI
Friedrich-Alexander University
Bifunctional compounds targeting both D2 and non-a7 nACh receptors: design, synthesis and pharmacological characterization.EBI
Universit£ degli Studi di Milano
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.EBI
Fudan University
Synthesis and evaluation of arylpiperazine-reverse amides as biased dopamine D3 receptor ligands.EBI
Chonnam National University
High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice.EBI
National Institute on Drug Abuse-Intramural Research Program
Structural manipulation on the catecholic fragment of dopamine D(1) receptor agonist 1-phenyl-N-methyl-benzazepines.EBI
Shanghai Institute of Materia Medica (SIMM)
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.EBI
National Institute on Drug Abuse-Intramural Research Program
Using click chemistry toward novel 1,2,3-triazole-linked dopamine D3 receptor ligands.EBI
National Institute on Drug Abuse-Intramural Research Program
Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding.EBI
Friedrich-Alexander-Universit£t Erlangen-N£rnberg
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.EBI
City University of New York
Molecular determinants of biased agonism at the dopamine D2 receptor.EBI
Friedrich-Alexander University
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.EBI
University of Illinois at Chicago
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI
Jagiellonian University Collegium Medicum
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.EBI
Northwestern University
Design, synthesis, and structure-activity relationship studies of a series of [4-(4-carboxamidobutyl)]-1-arylpiperazines: insights into structural features contributing to dopamine D3 versus D2 receptor subtype selectivity.EBI
Southern Research Institute
Further evaluation of the tropane analogs of haloperidol.EBI
Florida A&M University
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting▀2-adrenoceptor agonist.EBI
Novartis Institutes for BioMedical Research
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.EBI
Friedrich-Alexander University
Synthesis, pharmacological evaluation and molecular modeling studies of triazole containing dopamine D3 receptor ligands.EBI
Washington University
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.EBI
Universit£ degli Studi di Siena
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.EBI
Chinese Academy of Sciences
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.EBI
Vanderbilt University
Multiple fragment docking and linking in primary and secondary pockets of dopamine receptors.EBI
Gedeon Richter Plc
Chiral Resolution and Serendipitous Fluorination Reaction for the Selective Dopamine D3 Receptor Antagonist BAK2-66.EBI
National Institute on Drug Abuse-Intramural Research Program
Functionally selective dopamine D2, D3 receptor partial agonists.EBI
Friedrich-Alexander University
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI
Adamed Ltd.
Identification of a new selective dopamine D4 receptor ligand.EBI
Florida A&M University
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D3 receptor antagonists.EBI
University of Michigan
Antagonists of the kappa opioid receptor.EBI
The Scripps Research Institute
Thes2 receptor: a novel protein for the imaging and treatment of cancer.EBI
Washington University
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.EBI
National Center for Advancing Translational Sciences
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation.EBI
GlaxoSmithKline
Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers.EBI
Friedrich-Alexander University
Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety.EBI
Friedrich-Alexander University
Discovery of dopamine D4 receptor antagonists with planar chirality.EBI
Friedrich-Alexander University
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.EBI
Goethe University
Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT1A/5-HT2A/5-HT7 and dopamine D2/D3 receptors.EBI
Jagiellonian University Medical College
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.EBI
Janssen-Cilag S.A.
[3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists.EBI
GlaxoSmithKline
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.EBI
GlaxoSmithKline
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.EBI
Imperial College
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.EBI
Universidad de Santiago de Compostela
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part one: lead identification.EBI
Cancer Therapeutics
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.EBI
GlaxoSmithKline
Modulations of the amide function of the preferential dopamine D3 agonist (R,R)-S32504: improvements of affinity and selectivity for D3 versus D2 receptors.EBI
Institut de Recherches Servier
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.EBI
GlaxoSmithKline
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.EBI
GlaxoSmithKline
The role of QSAR in dopamine interactions.EBI
Pomona College
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI
SmithKline Beecham Pharmaceuticals Ltd
GRID/GOLPE 3D quantitative structure-activity relationship study on a set of benzamides and naphthamides, with affinity for the dopamine D3 receptor subtype.EBI
University Centre for Pharmacy
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.EBI
TBA
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.EBI
Janssen-Cilag S.A.
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.EBI
Janssen-Cilag S.A.
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).EBI
SmithKline Beecham Pharmaceuticals Ltd
Novel azulene derivatives for the treatment of erectile dysfunction.EBI
Friedrich-Alexander University
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.EBI
Savannah State University
Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach.EBI
NeuroSearch Sweden AB
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI
The University of Sydney
Synopsis of some recent tactical application of bioisosteres in drug design.EBI
Bristol-Myers Squibb Pharmaceutical Research and Development
Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.EBI
TBA
CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist.EBI
TBA
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.EBI
University of Innsbruck
A straightforward approach for engineering efficacy and selectivity at GPCRs.EBI
Universit£ degli Studi di Siena
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.EBI
National Institute on Drug Abuse-Intramural Research Program
Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D3 receptor-selective full agonist ligand.EBI
Purdue University
Structure-activity relationship study of N6-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine analogues: development of highly selective D3 dopamine receptor agonists along with a highly potent D2/D3 agonist and their pharmacological characterizatioEBI
Wayne State University
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI
TBA
High-affinity and selective dopamine D3 receptor full agonists.EBI
University of Michigan
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands.EBI
University of Tartu
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.EBI
The University of Sydney
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.EBI
National Institute of Mental Health
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.EBI
Gedeon Richter Plc
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.EBI
Harvard Medical School
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI
National Institute of Mental Health
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relaEBI
Pfizer Inc
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.EBI
H. Lundbeck A/S
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.EBI
Washington University
Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).EBI
Westfalische Wilhelms-Universitat
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI
Hunter College and the Graduate Center of the City University of New York
Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?EBI
Friedrich-Schiller-Universit£t Jena
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.EBI
Johann Wolfgang Goethe Universit£t
N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.EBI
National Institute on Drug Abuse-Intramural Research Program
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI
Purdue University
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.EBI
Clinic of Nuclear Medicine
Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET.EBI
Friedrich-Alexander University
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Multi-target-directed ligands to combat neurodegenerative diseases.EBI
University of Bologna
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.EBI
Janssen-Cilag S.A.
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.EBI
Purdue University
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.EBI
Laboratoire de Chimie Th�rapeutique
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.EBI
Organix Inc
Dopamine/serotonin receptor ligands. 10: SAR Studies on azecine-type dopamine receptor ligands by functional screening at human cloned D1, D2L, and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist.EBI
University of Bonn
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes for BioMedical Research
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.EBI
Friedrich-Alexander University
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.EBI
Wyeth Research
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.EBI
Friedrich-Alexander University
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.EBI
National Institute on Drug Abuse-Intramural Research Program
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.EBI
Brigham & Women's Hospital
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical Inc.
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction.EBI
Abbott Laboratories
Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.EBI
University of Michigan
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.EBI
H. Lundbeck A/S
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
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.EBI
Friedrich-Alexander University
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD).EBI
Purdue University
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.EBI
University of Groningen
Current and novel approaches to the drug treatment of schizophrenia.EBI
Merck Sharp and Dohme Research Laboratories
From hit to lead. Analyzing structure-profile relationships.EBI
Universities of Lille
Design and synthesis of [(2,3-dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as novel ligands selective for the dopamine D3 receptor subtype.EBI
National Institute on Drug Abuse-Intramural Research Program
Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.EBI
Friedrich-Alexander University
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.EBI
Friedrich-Alexander University
Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.EBI
University of Maastricht
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).EBI
University Centre for Pharmacy
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.EBI
Warner-Lambert Company
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.EBI
National Taiwan University
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI
Cooperation Pharmaceutique Fran�aise
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.EBI
Wyeth-Ayerst Research Laboratories
Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.EBI
University of Groningen
Synthesis and evaluation of pharmacological and pharmacokinetic properties of monopropyl analogs of 5-, 7-, and 8-[[(trifluoromethyl)sulfonyl]oxy]-2-aminotetralins: central dopamine and serotonin receptor activity.EBI
University of G£teborg
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.EBI
University of G£teborg
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.EBI
University of Pennsylvania
Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b ]-1,4-oxazin-7- and -9-ols: the significance of nitrogen pKa values for central dopamine receptor activation.EBI
State University of Groningen
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI
Virginia Commonwealth University
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.EBI
Friedrich-Alexander University
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.EBI
Friedrich-Alexander University
New generation dopaminergic agents. Part 8: heterocyclic bioisosteres that exploit the 7-OH-2-(aminomethyl)chroman D(2) template.EBI
Wyeth-Ayerst Research Laboratories
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.EBI
Friedrich-Alexander University
Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.EBI
Institute of Science and Technology
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).EBI
Friedrich-Alexander University
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.EBI
Friedrich-Alexander University
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.EBI
Universit£t Erlangen-N£rnberg
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.EBI
Universit£t Erlangen-N£rnberg
SAR of novel biarylmethylamine dopamine D4 receptor ligands.EBI
Darmstadt
 
Novel cyclohexyl amides as potent and selective D3 dopamine receptor ligandsEBI
TBA
Chiral indolo[3,2-f][3]benzazecine-type dopamine receptor antagonists: synthesis and activity of racemic and enantiopure derivatives.EBI
Martin-Luther-Universit£t Halle-Wittenberg
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.EBI
Florida A&M University
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI
Florida A&M University
Bivalent molecular probes for dopamine D2-like receptors.EBI
Friedrich-Alexander University
Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding.EBI
Forschungszentrum J£lich GmbH
Development of a bivalent dopamine D2 receptor agonist.EBI
Friedrich-Alexander University
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.EBI
The University of Mississippi
Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.EBI
Green Cross Corporation
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.EBI
Washington University
Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound.EBI
Washington University
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.EBI
Friedrich-Alexander University
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (s) receptor ligands modulates off-target activity and subtype selectivity.EBI
The University of Sydney
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.EBI
National Institute on Drug Abuse-Intramural Research Program
Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands.EBI
University of Santiago de Compostela
Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions.EBI
Friedrich-Alexander University
Synthesis and pharmacological evaluation of fluorine-containing D3 dopamine receptor ligands.EBI
Washington University
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands.EBI
Chinese Academy of Sciences
Biotin ergopeptide probes for dopamine receptors.EBI
University of Barcelona
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI
The University of Sydney
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.EBI
Korea Research Institute of Chemical Technology
Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET.EBI
Friedrich-Alexander-Universität Erlangen-Nürnberg
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.EBI
Friedrich-Alexander University
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.EBI
Friedrich-Alexander University
Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol.EBI
Wayne State University
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical and Public Health Institute
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.EBI
Purdue University
Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands.EBI
Université de Rennes I
Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: a novel series of atypical antipsychotic agents.EBI
Korea Research Institute of Chemical Technology
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI
Meiji Seika Kaisha, Ltd
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.EBI
Yangji Chemicals
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.EBI
Friedrich-Schiller-Universit£t Jena
Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI
Green Cross Corporation
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.EBI
Amgen Inc
Discovery of 4-(4-(2-((5-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)amino)ethyl)piperazin-1-yl)quinolin-8-ol and its analogues as highly potent dopamine D2/D3 agonists and as iron chelator: in vivo activity indicates potential application in symptomatic and neuroprotective therapy for ParkinEBI
Wayne State University
Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.EBI
Wayne State University
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.EBI
Wyeth Research
1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.EBI
Friedrich-Alexander University
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.EBI
Novartis Institutes for BioMedical Research
Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker.EBI
Friedrich-Alexander University
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.EBI
Friedrich-Alexander-Universit£t
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.EBI
Wyeth Research
Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.EBI
Wayne State University
Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding.EBI
Friedrich-Alexander University
 
Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptorEBI
TBA
 
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonistsEBI
TBA
 
A new series of selective dopamine D4 ligands: 3-([4-arylpiperazin-1-yl]alkylamino)-2H-1,4-benzoxazinesEBI
TBA
 
4-Heterocyclyl tetrahydropyridines as selective ligands for the human dopamine D4 receptorEBI
TBA
 
Discovery of selective dopamine D4 receptor antagonists: 1-Aryloxy-3-(4-aryloxypiperidinyl)-2-propanolsEBI
TBA
 
4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamides: Selective dopamine D3 receptor partial agonistsEBI
TBA
 
Discovery of selective dopamine D3 ligands: II. 2-[4-[3-(4-aryl-1-piperazinyl)propoxy]phenyl]benzimidazole partial agonistsEBI
TBA
 
Discovery of selective dopamine D3 ligands: I. Dimeric 2-[4-(3-aminopropoxy)phenyl]benzimidazole antagonistsEBI
TBA
 
Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic propertiesEBI
TBA
Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands.EBI
Universidad de Santiago de Compostela
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.EBI
Florida A&M University
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.EBI
Università degli Studi di Bari
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.EBI
University of Siena
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.EBI
Friedrich-Alexander University
Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.EBI
National Institute on Drug Abuses
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI
Merck Research Laboratories
Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists.EBI
Korea Research Institute of Chemical Technology
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.EBI
Florida A&M University
[11C]cyclopropyl-FLB 457: a PET radioligand for low densities of dopamine D2 receptors.EBI
Institutet
Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.EBI
Wayne State University
Further structure-activity relationships study of hybrid 7-{[2-(4-phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol analogues: identification of a high-affinity D3-preferring agonist with potent in vivo activity with long duration of action.EBI
Wayne State University
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.EBI
Korea Research Institute of Chemical Technology
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI
Pfizer Inc
4-[omega-[4-arylpiperazin-1-yl]alkoxy]phenyl)imidazo[1,2-a]pyridine derivatives: fluorescent high-affinity dopamine D3 receptor ligands as potential probes for receptor visualization.EBI
Università degli Studi di Bari
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.EBI
Friedrich-Alexander University
Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.EBI
Johann Wolfgang Goethe University
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.EBI
Johannes Gutenberg University
Dopamine/serotonin receptor ligands. 16.(1) Expanding dibenz[d,g]azecines to 11- and 12-membered homologues. Interaction with dopamine D(1)-D(5) receptors.EBI
Friedrich-Schiller-Universität Jena
Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.EBI
National Institute on Drug Abuse-Intramural Research Program
Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.EBI
Cairo University
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI
National Institute of Mental Health
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI
GlaxoSmithKline
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.EBI
Sungshin Women's University
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.EBI
Friedrich-Alexander University
Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.EBI
Friedrich-Schiller-Universität Jena
Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.EBI
National Institute on Drug Abuse-Intramural Research Program
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors.EBI
Friedrich-Schiller-Universität Jena
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.EBI
Friedrich-Alexander University
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI
Pfizer Inc
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.
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.EBI
Florida A&M University
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.EBI
Friedrich-Alexander University
Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist.EBI
Friedrich-Schiller-Universität Jena
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI
Columbia University College of Physicians and Surgeons
Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: variations on the 1H-pyrimidin-2-one theme.EBI
Abbott GmbH & Co. KG
Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors.EBI
Università degli Studi di Bari
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI
Columbia University College of Physicians and Surgeons
First structure-activity relationship study on dopamine D3 receptor agents with N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamide structure.EBI
Università degli Studi di Bari
Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.EBI
Abbott GmbH & Co. KG
Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com.EBI
Abbott GmbH & Co. KG
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.EBI
Abbott GmbH & Co. KG
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI
Columbia University College of Physicians and Surgeons
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.EBI
University of Erlangen-Nuremberg
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.EBI
7TM Pharma A/S
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.EBI
Friedrich-Alexander University
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.EBI
Janssen-Cilag S.A.
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.EBI
Johnson & Johnson Pharmaceutical Research & Development
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.EBI
Università di Siena
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.EBI
National Institute on Drug Abuse-Intramural Research Program
Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes.EBI
Friedrich-Alexander University
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.EBI
Wyeth Research
Indolebutylamines as selective 5-HT(1A) agonists.EBI
Merck KGaA
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.EBI
Friedrich-Schiller-Universität Jena
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.EBI
University of Erlangen-Nuremberg
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.EBI
Merck Research Laboratories
Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI
Virginia Commonwealth University
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.EBI
Neurogen Corporation
Structure-activity relationship of triaryl propionic acid analogues on the human EP3 prostanoid receptor.EBI
Merck Frosst Centre for Therapeutic Research
The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+.EBI
Florida A&M University
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.EBI
Friedrich-Alexander University
N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.EBI
Johann Wolfgang Goethe-Universität
Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.EBI
University of Sydney
N-(4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl, butenyl and butynyl)arylcarboxamides as novel dopamine D(3) receptor antagonists.EBI
National Institute on Drug Abuse-Intramural Research Program
Identification of a novel series of selective 5-HT7 receptor antagonists.EBI
GlaxoSmithKline
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.EBI
Friedrich-Alexander University
Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine.EBI
University Center for Pharmacy
A novel series of hybrid compounds derived by combining 2-aminotetralin and piperazine fragments: binding activity at D2 and D3 receptors.EBI
Wayne State University
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.EBI
Merck Sharp & Dohme Research Laboratories
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.EBI
Friedrich-Alexander University
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.EBI
GlaxoSmithKline
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).EBI
Friedrich-Alexander University
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HTEBI
City University of New York
Exploration of Alternative Scaffolds for P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors.EBI
Wyeth-Ayerst Research
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge EBI
University of Mississippi
Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands.EBI
Gedeon Richter Plc
Novel multifunctional dopamine DEBI
Wayne State University
Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.EBI
National Institute on Drug Abuse-Intramural Research Program
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.EBI
Jagiellonian University Medical College
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.EBI
The R. W. Johnson Pharmaceutical Research Institute
Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine DEBI
National Institute on Drug Abuse-Intramural Research Program
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.EBI
Marquette University
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.EBI
University of Siena
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI
National Institute of Neurological Disorders and Stroke
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.EBI
ShanghaiTech University
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.EBI
Friedrich-Alexander University
New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.EBI
Wyeth-Ayerst Research Laboratories
Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.EBI
Warner-Lambert Company
Rasagiline derivatives combined with histamine HEBI
Heinrich Heine University D£sseldorf
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
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI
University of Pennsylvania
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.EBI
Universität Erlangen - Nürnberg
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
Dopamine DEBI
Rowan University
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI
University of North Carolina at Chapel Hill
Chemical manipulations on the 1,4-dioxane ring of 5-HTEBI
Universit£ di Camerino
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI
University of Göteborg
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.EBI
Merck Sharp and Dohme Research Laboratories
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.EBI
Merck Sharp & Dohme Research Laboratories
Docking Finds GPCR Ligands in Dark Chemical Matter.EBI
Uppsala University
Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors.EBI
University of Vigo
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
Polypharmacology by Design: A Medicinal Chemist's Perspective on Multitargeting Compounds.EBI
Goethe University Frankfurt
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.EBI
Neurogen Corporation
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.EBI
Wyeth-Ayerst Research Laboratory
Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs.EBI
Medical University of Lublin
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.EBI
Parke-Davis Pharmaceutical Research
The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as DEBI
National Institute on Drug Abuse-Intramural Research Program
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.EBI
Wyeth-Ayerst Research Laboratories
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.EBI
Pfizer Inc
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine DEBI
Temple University School of Pharmacy
1-(2'-Bromobenzyl)-6,7-dihydroxy-EBI
Universidad de Santiago de Compostela
Aminopyrimidines with high affinity for both serotonin and dopamine receptors.EBI
Warner-Lambert Company
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.EBI
Warner-Lambert Company
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.EBI
Warner-Lambert Company
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.EBI
Merck Sharp and Dohme Research Laboratories
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.EBI
Warner-Lambert Company
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine DEBI
Friedrich-Alexander-Universit£t Erlangen-N£rnberg
Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.EBI
Pharmacia & Upjohn
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.EBI
Genentech
2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors.EBI
Neurogen Corporation
3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists.EBI
Division of Warner Lambert Company
Novel (R)-2-amino-5-fluorotetralins: dopaminergic antagonists and inverse agonists.EBI
Uppsala University
Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HTEBI
TBA
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University of Minnesota Twin Cities
Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.EBI
Warner-Lambert Company
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
Design, synthesis and evaluation of bitopic arylpiperazinephenyl-1,2,4-oxadiazoles as preferential dopamine D3 receptor ligands.EBI
Chonnam National University
Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.EBI
Wayne State University
Identification, characterization and pharmacological profile of three metabolites of (R)-(+)-1,2,3,6-tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1- yl)methyl]pyridine (CI-1007), a dopamine autoreceptor agonist and potential antipsychotic agent.EBI
Warner-Lambert Company
Synthesis and EBI
Washington University School of Medicine
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.EBI
University of Göteborg
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.EBI
University of Pennsylvania
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.EBI
Parke-Davis Pharmaceutical Research
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.EBI
Warner-Lambert Company
Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin.EBI
Warner-Lambert Company
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory AS
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.EBI
GlaxoSmithKline
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.EBI
Solvay Pharma
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.EBI
GlaxoSmithKline
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.EBI
GlaxoSmithKline
Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species.EBI
Florida A and M University
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.EBI
GlaxoSmithKline Pharmaceuticals
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.EBI
Glaxo Research and Development Ltd.
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI
Huazhong University of Science and Technology
New Dopamine D3-Selective Receptor Ligands Containing a 6-Methoxy-1,2,3,4-tetrahydroisoquinolin-7-ol Motif.EBI
City University of New York
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI
Texas Tech University Health Sciences Center
Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine DEBI
Southern Illinois University Edwardsville
Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
University of Texas at Austin
N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride.EBI
Washington University
Development of molecular tools based on the dopamine DEBI
Friedrich-Alexander University
Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine DEBI
National Institute on Drug Abuse
Toward Understanding the Structural Basis of Partial Agonism at the Dopamine DEBI
National Institute on Drug Abuse-Intramural Research Program
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DEBI
Universit£ di Camerino
?-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.EBI
Friedrich-Alexander University Erlangen-N£rnberg
Potent haloperidol derivatives covalently binding to the dopamine D2 receptor.EBI
Friedrich-Alexander University Erlangen-N£rnberg
Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening.EBI
Bioprojet-Biotech
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HTEBI
Universit£ di Camerino
Return of DEBI
University of Nebraska Medical Center
Highly Selective Dopamine DEBI
University of Pennsylvania
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for?-Arrestin-Biased DEBI
Friedrich-Alexander University Erlangen-Nuernberg
Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII.BDB
Vilnius University
Synthesis, inhibitory activity and molecular docking studies of two Cu(II) complexes against Helicobacter pylori urease.BDB
Wuhan Textile University
Steroidal 5a-reductase inhibitors using 4-androstenedione as substrate.BDB
Metropolitan University-Xochimilco
Talaromyces marneffei Mp1p Is a Virulence Factor that Binds and Sequesters a Key Proinflammatory Lipid to Dampen Host Innate Immune Response.BDB
The University of Hong Kong
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
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.BDB
Chulabhorn Research Institute
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
Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.BDB
Birla Institute of Technology
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.BDB
Tehran University of Medical Sciences
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University of Leipzig
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).BDB
Oregon Health & Science University
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.BDB
Gwangju Institute of Science and Technology
Radioreceptor binding profile of the atypical antipsychotic olanzapine.BDB
Eli Lilly and Company
Competition of leukotrienes and ICI-198,615 for [3H]LTD4 binding sites in guinea pig lung membranes suggests the involvement of two LTD4 receptor subtypes.BDB
Pfizer Inc
Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.BDB
Wyeth Research