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532 articles for thisTarget


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

PMID
Data
Article Title
Organization
Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.EBI
Friedrich-Alexander University Erlangen-N£Rnberg
Asymmetric total synthesis of tetrahydroprotoberberine derivatives and evaluation of their binding affinities at dopamine receptors.EBI
Harvard Medical School
Conformational analysis and molecular modeling of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as D1 dopamine receptor ligands.EBI
University of North Carolina
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
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University of Kansas
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
Structure-guided development of dualß2 adrenergic/dopamine D2 receptor agonists.EBI
Friedrich-Alexander University
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
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity.EBI
City University of New York
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.EBI
Dipartimento Di Farmacia Universit£
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI
Aptuit
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.EBI
City University of New York
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
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.EBI
Fudan University
Structural manipulation on the catecholic fragment of dopamine D(1) receptor agonist 1-phenyl-N-methyl-benzazepines.EBI
Shanghai Institute of Materia Medica (Simm)
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
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors.EBI
University of Barcelona
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.EBI
Boehringer Ingelheim (Canada)
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI
Jagiellonian University Collegium Medicum
Further evaluation of the tropane analogs of haloperidol.EBI
Florida A&M University
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.EBI
Friedrich-Alexander University
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
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.EBI
Novartis Institutes For Biomedical Research
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.EBI
Vanderbilt University
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
Identification of a new selective dopamine D4 receptor ligand.EBI
Florida A&M University
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.EBI
State Key Laboratory of Drug Research
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.EBI
Intra-Cellular Therapies
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.EBI
University of Santiago De Compostela
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
Design and synthesis of D1 agonist/D2 antagonist for treatment of schizophrenia.EBI
Sanofi Us
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.EBI
Chinese Academy of Sciences
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.EBI
Goethe University
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.EBI
Universidad De Santiago De Compostela
Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors.EBI
Friedrich-Schiller-Universit£T Jena
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.EBI
University of Li£Ge
Novel azulene derivatives for the treatment of erectile dysfunction.EBI
Friedrich-Alexander University
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
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI
Universite£
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.EBI
University of Innsbruck
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI
Sanford-Burnham Medical Research Institute
Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D3 receptor-selective full agonist ligand.EBI
Purdue University
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands.EBI
University of Tartu
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor.EBI
Shenyang Pharmaceutical University
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors.EBI
Shanghai Institute of Pharmaceutical Industry
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI
Amgen
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
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.EBI
University of Namur
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
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.EBI
Aska Pharmaceutical
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
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.EBI
Chinese Academy of Sciences
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
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)
'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity.EBI
Chinese Academy of Sciences
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
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.EBI
Egis Pharmaceuticals
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.EBI
Harvard Medical School
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 novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol.EBI
University Centre For Pharmacy
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Advances in development of dopaminergic aporphinoids.EBI
Chinese Academy of Sciences
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.EBI
Abbott Laboratories
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
University of Tours
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.EBI
Organix
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.EBI
Pfizer
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
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
University of Urbino
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
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.EBI
Friedrich-Alexander University
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
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
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
University of Siena
New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor.EBI
University of Pisa
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.EBI
Friedrich-Alexander University
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.EBI
University of Siena
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
Current and novel approaches to the drug treatment of schizophrenia.EBI
Merck Sharp and Dohme Research Laboratories
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.EBI
Eli Lilly
From hit to lead. Analyzing structure-profile relationships.EBI
Universities of Lille
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
7-Methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine: a new heterocyclic system and a new lead compound for dopamine receptor antagonists.EBI
University of Bonn
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.EBI
Taisho Pharmaceutical
N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies.EBI
University of Pisa
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.EBI
University of Minnesota
CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors.EBI
University of Texas At Austin
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.EBI
University of Crete
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.EBI
Universita' Di Siena
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.EBI
Astra Arcus
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.EBI
Cooperation Pharmaceutique Fran�Aise
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.EBI
Abbott Laboratories
Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors.EBI
Va Medical Center
Synthesis, resolution, and preliminary evaluation of trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes and related derivatives as dopamine receptors ligands.EBI
University of Camerino
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
(+/-)-(N-alkylamino)benzazepine analogs: novel dopamine D1 receptor antagonists.EBI
National Institutes of Health
(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
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.EBI
Albany Molecular Research
3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies.EBI
Orleans University
Synthesis and pharmacological evaluation of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for a novel receptor with sigma-like neuromodulatory activity.EBI
University of North Carolina
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.EBI
Searle Research and Development
A study on the contribution of the 1-phenyl substituent to the molecular electrostatic potentials of some benzazepines in relation to selective dopamine D-1 receptor activity.EBI
University of Lund
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
Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands.EBI
University of Camerino
Novel piperidine sigma receptor ligands as potential antipsychotic drugs.EBI
Dupont Pharmaceuticals
(+/-)-3-allyl-7-halo-8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines as selective high affinity D1 dopamine receptor antagonists: synthesis and structure-activity relationship.EBI
Northeastern University
Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.EBI
Warner-Lambert
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.EBI
Virginia Commonwealth University
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.EBI
Hoechst-Roussel Pharmaceuticals
(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship.EBI
Northeastern University
Fluorescent probes for dopamine receptors: synthesis and characterization of fluorescein and 7-nitrobenz-2-oxa-1,3-diazol-4-yl conjugates of D-1 and D-2 receptor ligands.EBI
Research Biochemicals
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.EBI
Abbott Laboratories
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.EBI
Warner-Lambert
R and S enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue.EBI
Northeastern University
Synthesis and dopamine receptor affinities of 2-(4-fluoro-3- hydroxyphenyl)ethylamine and N-substituted derivatives.EBI
University of Camerino
Conformational analysis and structure-activity relationships of selective dopamine D-1 receptor agonists and antagonists of the benzazepine series.EBI
Royal Danish School of Pharmacy
trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist.EBI
Purdue University
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.EBI
Abbott Laboratories
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.EBI
Pfizer
Synthesis and structural requirements of N-substituted norapomorphines for affinity and activity at dopamine D-1, D-2, and agonist receptor sites in rat brain.EBI
Northeastern University
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.EBI
Warner-Lambert
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.EBI
University of G£Teborg
A photoaffinity label for the D-1 dopamine receptor, (RS)-7-[125I]Iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5- tetrahydro-1H-3-benzazepine, selectively identifies the ligand binding subunits of the receptor.EBI
Northeastern University
Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands.EBI
University of North Carolina
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.EBI
TBA
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.EBI
Istituto Superiore Di Sanit£
Dopamine agonists related to 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzaz epi ne-7, 8-diol. 6-Position modifications.EBI
TBA
Synthesis and dopaminergic binding of 2-aryldopamine analogues: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes.EBI
TBA
Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics.EBI
TBA
(+/-)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
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.EBI
Friedrich-Alexander University
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.EBI
Abbott Laboratories
Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand.EBI
University of Pisa
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
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.EBI
Yale 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
 
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibitionEBI
TBA
 
Dopamine autoreceptor agonists: computational studies, synthesis and biological investigationsEBI
TBA
 
Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385EBI
TBA
 
Novel 4,5,6,7-tetrahydrobenzothiazole dopamine agonists display very low stereoselectivity in their interaction with dopamine receptors.EBI
TBA
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
University of Siena
First enantioselective syntheses of the dopamine D1 and D2 receptor modulators, (+)- and (-)-govadine.EBI
University of British Columbia
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
Analogues of doxanthrine reveal differences between the dopamine D1 receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a]phenanthridines.EBI
Quimique C£A.
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.EBI
University of Naples Federico II
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
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
Assessment of dopamine D¿? receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393.EBI
Purdue University
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI
The University of Sydney
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.EBI
Soochow University College of Pharmaceutical Sciences
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.EBI
Friedrich-Alexander University
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists.EBI
University of Tartu
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.EBI
University of Naples Federico II
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
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
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands.EBI
Chinese Academy of Sciences
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
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.EBI
Bristol-Myers Squibb
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
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI
National Institute of Mental Health
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
Smoothened antagonists for hair inhibition.EBI
Pfizer
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI
Università
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.EBI
Universita Di Siena
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
New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation.EBI
University of Naples Federico II
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.EBI
Friedrich-Schiller-Universit£T Jena
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.EBI
Merck Research Laboratories
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.EBI
Merck Research Laboratories
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.EBI
Schering-Plough Research Institute
Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.EBI
University of Naples Federico II
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
N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists.EBI
University of Tartu
Displacement Activity of Bisbenzylisoquinoline Alkaloids at Striatal 3H-SCH 23390 and 3H-Raclopride Binding SitesEBI
TBA
The Role of Receptor Binding in Drug DiscoveryEBI
TBA
 
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamidesEBI
TBA
 
(E) and (Z)-3-Styrylpiperidines as sigma ligandsEBI
TBA
 
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI
TBA
 
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)EBI
TBA
 
Novel HO-DPAT (hydroxy-2-dipropylaminotetralin) isomers: Stereoselective synthesis and receptor binding studiesEBI
TBA
 
Dopamine receptor binding properties of some 2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols with non-aromatic substituents in the 5-positionEBI
TBA
 
Synthesis and evaluation of several cathechol bioisosteres as potential dopamine receptor ligandsEBI
TBA
 
Synthesis and dopaminergic activity of the enantiomers of 6-methyl-4,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine (PD 128483).EBI
TBA
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)
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.EBI
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz
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
Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.EBI
Harvard Medical School
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.EBI
Chinese Academy of Sciences
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.EBI
Friedrich-Alexander University
Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile.EBI
University of Michigan
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.EBI
Chinese Academy of Sciences
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 of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.EBI
Università
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
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.EBI
Harvard Medical School
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines.EBI
Chinese Academy of Sciences
Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines.EBI
University of Debrecen
Synthesis, binding properties and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl)ethyl]-1H-benzimidazoles, mixed ligands of D2 and 5-HT1A receptors.EBI
University of Belgrade
Halogenated boldine derivatives with enhanced monoamine receptor selectivity.EBI
Universidad De Chile
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.EBI
Universidad De Valencia
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
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.EBI
Friedrich-Alexander 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
Transformation of a Dopamine DEBI
Shanghaitech 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
Dopamine DEBI
National Institute On Drug Abuse?Intramural Research Program
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.EBI
Harvard Medical School
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.EBI
Institut D'Investigacions BiomèDiques August Pi I
Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine DEBI
Kindai University
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists.EBI
Friedrich-Alexander-Universitat Erlangen-Nurnberg
Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.EBI
Tianjin University
Novel sigma receptor ligands: synthesis and biological profile.EBI
University of Catania
Targeting σEBI
The University of Texas At Austin
Discovery of Selective Dopamine Receptor Ligands Derived from (-)-Stepholidine via C-3 Alkoxylation and C-3/C-9 Dialkoxylation.EBI
City University of New York
Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.EBI
Friedrich-Alexander University
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.EBI
High Point University
Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.EBI
University of Michigan
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
From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.EBI
University of Nebraska Medical Center
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
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.EBI
Schering-Plough Research Institute
Modification of the clozapine structure by parallel synthesis.EBI
Schering-Plough Research Institute
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
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
Abolishing Dopamine DEBI
University of Regensburg
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
Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists.EBI
University of Nebraska Medical Center
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
3-Arylpiperazinylethyl-1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione derivatives as novel, high-affinity and selective alpha(1)-adrenoceptor ligands.EBI
Università
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
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.EBI
Università
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.EBI
Zhejiang University
2-(Fluoromethoxy)-4'-(EBI
Universidad Complutense De Madrid
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.EBI
H. Lundbeck
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.EBI
Friedrich-Alexander University
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.EBI
Università
Research progress in biological activities of isochroman derivatives.EBI
Shaanxi University of Chinese Medicine
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
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.EBI
TBA
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
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
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators.EBI
Pfizer
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.EBI
University of Erlangen-Nuremberg
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.EBI
Pfizer
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.EBI
Wyeth Research
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DEBI
Shanghaitech University
New tetrahydroisoquinoline-based DEBI
City University of New York
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.EBI
Cracow University of Technology
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.EBI
Neurogen
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.EBI
Yale University
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.EBI
Sumitomo Dainippon Pharma.
Orally active oxime derivatives of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one. Synthesis and pharmacological activity.EBI
University Center For Pharmacy
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.EBI
Friedrich-Alexander University
Structure-Activity Relationship of Heterocyclic P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine DEBI
National Institute On Drug Abuse-Intramural Research Program
Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity.EBI
University Centre For Pharmacy
New benzo[h][1,6]naphthyridine and azepino[3,2-c]quinoline derivatives as selective antagonists of 5-HT4 receptors: binding profile and pharmacological characterization.EBI
Université
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725.EBI
Friedrich-Alexander University
Isoquinolinone derivatives as potent CNS multi-receptor DEBI
Jiangsu Ocean University
The Essential Medicinal Chemistry of Cannabidiol (CBD).EBI
University of Minnesota
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.EBI
Pharmazeutisches Institut Der UniversitäT Freiburg
Development of pyrimidone D1 dopamine receptor positive allosteric modulators.EBI
National Institutes of Health
Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine DEBI
Sumitomo Dainippon Pharma.
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.EBI
Friedrich-Alexander University
Identification of C10 nitrogen-containing aporphines with dopamine DEBI
City University of New York
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
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines.EBI
City University of New York
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI
Columbia University College of Physicians and Surgeons
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.EBI
Universidad De Valencia
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.EBI
University of Crete
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge EBI
University of Mississippi
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.EBI
University of Texas Medical Branch
Synthesis of novel 5-substituted 3-amino-3,4-dihydro-2H-1-benzopyran derivatives and their interactions with the 5-HT1A receptor.EBI
Astrazeneca R&D SöDertäLje
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.EBI
University of Tokyo
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
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
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI
University of North Carolina At Chapel Hill
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI
University of GöTeborg
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.EBI
Postech
trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists.EBI
Abbott Laboratories
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
Novel Strategies To Activate the Dopamine DEBI
Ucb Pharma
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.EBI
Shanghaitech University
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.EBI
Neurogen
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
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI
Rti International
Serotonergic ergoline derivatives.EBI
Pharmacia & Upjohn
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.EBI
R. W. Johnson Pharmaceutical Research Institute
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine DEBI
Temple University
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.EBI
Duke University
Chemical synthesis, microbial transformation and biological evaluation of tetrahydroprotoberberines as dopamine D1/D2 receptor ligands.EBI
Huzhou University
Novel Pyrazolyl-dihydroisoquinolines as Positive Allosteric Modulator of the Dopamine D1 Receptor.EBI
Arrival Discovery
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1EBI
Amri
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI
University of Groningen
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prEBI
Abbott Laboratories
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine DEBI
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.EBI
Università
3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]EBI
Université
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI
University of Minnesota Twin Cities
11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.EBI
Uppsala University
10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.EBI
Uppsala University
(+/-)-3-[4'-(N,N-dimethylamino)cinnamyl]benzazepine analogs: novel dopamine D1 receptor antagonists.EBI
National Institutes of Health
Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.EBI
Warner-Lambert
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.EBI
Yamanouchi Pharmaceutical
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.EBI
Pharmacia & Upjohn
Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping.EBI
University of North Carolina
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
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI
Janssen Pharmaceutica
A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds.EBI
University of Lund
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.EBI
Eli Lilly
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.EBI
Virginia Commonwealth University
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.EBI
University of LièGe
Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.EBI
Vanderbilt University
2,3,9- and 2,3,11-trisubstituted tetrahydroprotoberberines as D2 dopaminergic ligands.EBI
Universidad De Valencia
Synthesis and molecular modeling of 1-phenyl-1,2,3,4-tetrahydroisoquinolines and related 5,6,8,9-tetrahydro-13bH-dibenzo[a,h]quinolizines as D1 dopamine antagonists.EBI
University of North Carolina
3,4-Dihydroxy- and 3,4-methylenedioxy- phenanthrene-type alkaloids with high selectivity for D2 dopamine receptor.EBI
Universidad De Valencia
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
Dopaminergic benzo[a]phenanthridines: resolution and pharmacological evaluation of the enantiomers of dihydrexidine, the full efficacy D1 dopamine receptor agonist.EBI
Purdue University
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.EBI
R. W. Johnson Pharmaceutical Research Institute
(R)-11-hydroxy- and (R)-11-hydroxy-10-methylaporphine: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.EBI
Uppsala University
Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands.EBI
Purdue University
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.EBI
Wellcome Research Laboratories
Synthesis and evaluation of 6,7-dihydroxy-2,3,4,8,9,13b-hexahydro-1H- benzo[6,7]cyclohepta[1,2,3-ef][3]benzazepine, 6,7-dihydroxy- 1,2,3,4,8,12b-hexahydroanthr[10,4a,4-cd]azepine, and 10-(aminomethyl)-9,10- dihydro-1,2-dihydroxyanthracene as conformationally restricted analogs of beta-phenyldopaminEBI
Purdue University
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.EBI
H. Lundbeck
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI
Drug Discovery Laboratory
Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent.EBI
Central Drug Research Institute
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.EBI
University of Camerino
Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.EBI
Universidad De Santiago
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.EBI
Monash University
(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity.EBI
Sandoz Pharma
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.EBI
University of Santiago De Compostela
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.EBI
Glaxo Research and Development
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
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.EBI
Pfizer
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.EBI
Texas Tech University Health Sciences Center
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.EBI
Northeastern University
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
Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent benzothiazol-2-one 7-ethylamines.EBI
TBA
Substituted benzamides with conformationally restricted side chains. 2. Indolizidine derivatives as central dopamine receptor antagonists.EBI
Beecham Pharmaceuticals Research Division
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.EBI
Warner-Lambert
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents.EBI
Warner-Lambert/Parke-Davis Pharmaceutical Research
New 5-HTEBI
Dipartimento Di Farmacia Universit£
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI
University of Texas At Austin
Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol.EBI
Schering-Plough
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.EBI
Mcneil Pharmaceutical and Janssen Research Foundation Worldwide
(+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent.EBI
University of Pennsylvania
Aporphines as antagonists of dopamine D-1 receptors.EBI
Eli Lilly
Development of a high affinity and stereoselective photoaffinity label for the D-1 dopamine receptor: synthesis and resolution of 7-[125I]iodo-8-hydroxy-3-methyl-1-(4'-azidophenyl)-2,3,4,5-tetrahydro- 1H-3-benzazepine.EBI
Research Biochemicals
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.EBI
Janssen Infectious Diseases-Diagnostics
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.EBI
Phenex Pharmaceuticals
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.EBI
Research Biochemicals
Development of molecular tools based on the dopamine DEBI
Friedrich-Alexander University
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.EBI
Northeastern University
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.EBI
Vanderbilt University
β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.EBI
Friedrich-Alexander University Erlangen-N£Rnberg
Return of DEBI
University of Nebraska Medical Center
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.EBI
Pfizer
Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists.EBI
H. Lundbeck
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.EBI
Harvard Medical School
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.EBI
Virginia Commonwealth University
Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.EBI
Virginia Commonwealth University
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
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.EBI
University of Catania
Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analogue.EBI
Research Biochemicals
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.EBI
Hoechst-Roussel Pharmaceuticals
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds forβ-Arrestin-Biased DEBI
Friedrich-Alexander University Erlangen-Nuernberg
RNA virus inhibitor compounds and uses thereofBDB
University of Alberta
NOVEL COMPOUNDSBDB
Sitryx Therapeutics
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATIONBDB
Genentech
MACROCYCLIC PEPTIDOMIMETIC PROTEASE INHIBITOR AND USE THEREOFBDB
Tencent Technology (Shenzhen)
Indazole carboxamides as kinase inhibitorsBDB
Bristol-Myers Squibb
SELECTIVE MODULATORS OF ATAXIA TELANGIECTASIA MUTATED (ATM) KINASE AND USES THEREOFBDB
Suzhou Zanrong Pharma
COMPOUND AS BRAIN-PERMEABLE BTK OR HER2 INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOFBDB
Chengdu Hyperway Pharmaceuticals
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetesBDB
Sprint Bioscience
LDHA activity inhibitorsBDB
Arctic Pharma
N-((HET)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitorsBDB
Kalvista Pharmaceuticals
Compounds as rearranged during transfection (RET) inhibitorsBDB
Glaxosmithkline Intellectual Property Development
Indane-amines as PD-L1 antagonistsBDB
Chemocentryx
Heterocyclic inhibitors of monocarboxylate transporterBDB
The Scripps Research Institute
Ethyldiamine orexin receptor antagonistsBDB
Merck Sharp & Dohme
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitorsBDB
Ctxt
Methods of use of cyclopamine analogsBDB
Infinity Pharmaceuticals
Inhibitors of PTP4A3 for the treatment of cancerBDB
University of Virginia Patent Foundation
Compounds and compositions for inhibiting the activity of SHP2BDB
Novartis
Tricyclic heterocyclic compounds useful as inhibitors of TNFBDB
Bristol-Myers Squibb
Fucosidase inhibitorsBDB
Horizon Orphan
Therapeutic compounds and compositions, and methods of use thereofBDB
Genentech
Pyridinyl and fused pyridinyl triazolone derivativesBDB
Takeda Pharmaceutical
Compounds for the inhibition of cyclophilins and uses thereofBDB
Merck Patent
Heteroaromatic compounds as BTK inhibitorsBDB
Boehringer Ingelheim International
Urea and amide derivatives of aminoalkylpiperazines and use thereofBDB
Southern Research Institute
Morphinan derivativeBDB
University of Tsukuba
Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereofBDB
Taiho Pharmaceutical
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivativesBDB
Idorsia Pharmaceuticals
Styryl quinazoline derivatives as pharmaceutically active agentsBDB
Vichem Chemie Kutató
Oxazoline and isoxazoline derivatives as CRAC modulatorsBDB
Lupin
Compounds as rearranged during transfection (RET) inhibitorsBDB
Glaxosmithkline
C-ring modified tricyclic benzonaphthiridinone protein kinase inhibitors and use thereofBDB
Merck Patent
Isoquinolin-3-yl carboxamides and preparation and use thereofBDB
Samumed
Morphan and morphinan analogues, and methods of useBDB
Alkermes Pharma Ireland
Pyridazinone compounds and their use as DAAO inhibitorsBDB
Takeda Pharmaceutical
Syk inhibitorsBDB
Gilead Sciences
Salt of fused pyrimidine compound and crystal thereofBDB
Taiho Pharmaceutical
Inhibitors of plasma kallikreinBDB
Kalvista Pharmaceuticals
Non-annulated thiophenylamidesBDB
Hoffmann-La Roche
Synthesis and biological activity of progesterone derivatives as 5alpha-reductase inhibitors, and their effect on hamster prostate weight.BDB
Universidad Nacional Autonoma De Mexico
Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's diseaseBDB
University of Kansas
Structural determinants of Tau aggregation inhibitor potency.BDB
The Ohio State University
1,3,5-triazine-2-amine derivatives, preparation thereof and diagnostic and therapeutic use thereofBDB
Sanofi
5-alkynyl-pyridinesBDB
Boehringer Ingelheim International
Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors.BDB
University of Karachi
Chymase inhibitorsBDB
Boehringer Ingelheim International
Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli.BDB
Astrazeneca India
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetesBDB
Merck Sharpe & Dohme
Inhibition of AcpA phosphatase activity with ascorbate attenuates Francisella tularensis intramacrophage survival.BDB
University of Florida
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.BDB
National Cancer Institute-Frederick
SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation.BDB
Sanofi-Synthelabo Research
Novel cyclic peptide agonist of high potency and selectivity for the type II vasoactive intestinal peptide receptor.BDB
University of California San Francisco
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.BDB
Vertex Pharmaceuticals
DcpS as a therapeutic target for spinal muscular atrophy.BDB
Decode Chemistry
A new screening assay for allosteric inhibitors of cSrc.BDB
Chemical Genomics Centre of The Max Planck Society
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.BDB
The Scripps Research Institute
Identification of RIP1 kinase as a specific cellular target of necrostatins.BDB
Tufts University
Splicing factor SF3b as a target of the antitumor natural product pladienolide.BDB
Eisai
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.BDB
University of Cambridge
 
Calorimetric Studies on the Complexation of Several Ferrocene Derivatives by .alpha.- and .beta.-Cyclodextrin. Effects of Urea on the Thermodynamic ParametersBDB
University of Miami
 
Chiral Recognition Thermodynamics of β-Cyclodextrin: The Thermodynamic Origin of Enantioselectivity and the Enthalpy-Entropy Compensation EffectBDB
Japan Science and Technology Agency
Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.BDB
Virginia Commonwealth University
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.BDB
Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.BDB
Vernalis (R&D)
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.BDB
Wyeth Research
Biarylether amide quinolines as liver X receptor agonists.BDB
Wyeth Research
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.BDB
Duquesne University
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.BDB
University of Alabama At Birmingham
Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.BDB
Cnrs
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.BDB
Johnson & Johnson Pharmaceutical
Compounds binding to the S2-S3 pockets of thrombin.BDB
University of Kalmar
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.BDB
Bristol-Myers Squibb
Chalcones: a valid scaffold for monoamine oxidases inhibitors.BDB
Sapienza University of Rome
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.BDB
Universita Del Piemonte Orientale
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.BDB
Bristol-Myers Squibb
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.BDB
Wyeth Research
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.BDB
Absolute Science
1-Sulfonylindazoles as potent and selective 5-HT6 ligands.BDB
Wyeth Research
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.BDB
Nerviano Medical Sciences
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.BDB
Gsk
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.BDB
Abbott Laboratories
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.BDB
Schering-Plough Research Institute
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.BDB
Valeant Pharmaceuticals Research and Development
Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors.BDB
University of Southern California
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.BDB
Burnham Institute For Medical Research
The molecular interactions of buspirone analogues with the serotonin transporter.BDB
National Medicines Institute
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).BDB
Saarland University
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.BDB
Sunesis Pharmaceuticals
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.BDB
Monash University
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.BDB
Purdue University
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.BDB
Astrazeneca
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.BDB
Irbm/Merck Research Laboratories
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.BDB
Novartis
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase.BDB
Bryn Mawr College
Structure of the BH3 domains from the p53-inducible BH3-only proteins Noxa and Puma in complex with Mcl-1.BDB
University of Otago