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Article Title
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Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.

Friedrich-Alexander University Erlangen-N£Rnberg
Asymmetric total synthesis of tetrahydroprotoberberine derivatives and evaluation of their binding affinities at dopamine receptors.

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.

University of North Carolina
Synthesis and evaluation of C9 alkoxy analogues of (-)-stepholidine as dopamine receptor ligands.

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-CH

Jagiellonian University Medical College
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.

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.

Aptuit
Structure-guided development of dualß2 adrenergic/dopamine D2 receptor agonists.

Friedrich-Alexander University
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.

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.

Jagiellonian University Medical College
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity.

City University of New York
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.

Dipartimento Di Farmacia Universit£
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.

Aptuit
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.

City University of New York
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.

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.

Friedrich-Alexander University
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.

Fudan University
Structural manipulation on the catecholic fragment of dopamine D(1) receptor agonist 1-phenyl-N-methyl-benzazepines.

Shanghai Institute of Materia Medica (Simm)
Fluoro-substituted phenylazocarboxamides: Dopaminergic behavior and N-arylating properties for irreversible binding.

Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors.

City University of New York
Molecular determinants of biased agonism at the dopamine D2 receptor.

Friedrich-Alexander University
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors.

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.

Boehringer Ingelheim (Canada)
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.

Jagiellonian University Collegium Medicum
Further evaluation of the tropane analogs of haloperidol.

Florida A&M University
Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D(2)-like receptors.

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.

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.

Novartis Institutes For Biomedical Research
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.

Vanderbilt University
Functionally selective dopamine D2, D3 receptor partial agonists.

Friedrich-Alexander University
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.

Adamed
Identification of a new selective dopamine D4 receptor ligand.

Florida A&M University
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.

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.

Intra-Cellular Therapies
Synthesis and antidopaminergic activity of some 3-(aminomethyl)tetralones as analogues of butyrophenone.

University of Santiago De Compostela
Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers.

Friedrich-Alexander University
Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety.

Friedrich-Alexander University
Discovery of dopamine D4 receptor antagonists with planar chirality.

Friedrich-Alexander University
Design and synthesis of D1 agonist/D2 antagonist for treatment of schizophrenia.

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.

Chinese Academy of Sciences
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.

Goethe University
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.

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.

Friedrich-Schiller-Universit£T Jena
Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study.

University of Li£Ge
Novel azulene derivatives for the treatment of erectile dysfunction.

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).

The University of Sydney
Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research and Development
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.

Universite£
Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective¿ opioid receptor agonist.

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.

Sanford-Burnham Medical Research Institute
Identification of a 2-phenyl-substituted octahydrobenzo[f]quinoline as a dopamine D3 receptor-selective full agonist ligand.

Purdue University
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands.

University of Tartu
Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: selective inhibitors of dopamine D1 receptor.

Shenyang Pharmaceutical University
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors.

Shanghai Institute of Pharmaceutical Industry
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.

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.

National Institute of Mental Health
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.

Gedeon Richter
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.

University of Namur
Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.

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.

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 rela

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.

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.

H. Lundbeck
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.

Chinese Academy of Sciences
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.

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?

Friedrich-Schiller-Universit£T Jena
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.

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.

Chinese Academy of Sciences
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics.

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.

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.

Purdue University
(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.

Egis Pharmaceuticals
Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.

Harvard Medical School
Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker.

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.

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.

University Centre For Pharmacy
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories
Advances in development of dopaminergic aporphinoids.

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.

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.

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.

University of Tours
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.

Organix
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.

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.

University of Bonn
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.

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.

University of Urbino
Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists.

Friedrich-Alexander University
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.

Friedrich-Alexander University
Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.

Brigham & Women'S Hospital
Selective optimization of side activities: another way for drug discovery.

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.

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.

University of Siena
New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor.

University of Pisa
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.

Friedrich-Alexander University
Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies.

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).

Purdue University
Current and novel approaches to the drug treatment of schizophrenia.

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.

Eli Lilly
From hit to lead. Analyzing structure-profile relationships.

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.

Friedrich-Alexander University
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.

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.

University of Bonn
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.

Taisho Pharmaceutical
N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies.

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.

University of Minnesota
CoMFA-based prediction of agonist affinities at recombinant D1 vs D2 dopamine receptors.

University of Texas At Austin
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.

University of Crete
New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure.

Universita' Di Siena
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.

Astra Arcus
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.

Cooperation Pharmaceutique Fran�Aise
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.

Abbott Laboratories
Comparative molecular field analysis-based prediction of drug affinities at recombinant D1A dopamine receptors.

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.

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).

Hoechst-Roussel Pharmaceuticals
(+/-)-(N-alkylamino)benzazepine analogs: novel dopamine D1 receptor antagonists.

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).

Abbott Laboratories
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.

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.

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.

University of North Carolina
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.

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.

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.

Bristol-Myers Squibb
Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl)ethylamine and N,N-dialkyl derivatives as dopamine receptor ligands.

University of Camerino
Novel piperidine sigma receptor ligands as potential antipsychotic drugs.

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.

Northeastern University
Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.

Warner-Lambert
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.

Virginia Commonwealth University
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.

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.

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.

Research Biochemicals
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.

Abbott Laboratories
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.

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.

Northeastern University
Synthesis and dopamine receptor affinities of 2-(4-fluoro-3- hydroxyphenyl)ethylamine and N-substituted derivatives.

University of Camerino
Conformational analysis and structure-activity relationships of selective dopamine D-1 receptor agonists and antagonists of the benzazepine series.

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.

Purdue University
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.

Abbott Laboratories
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

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.

Northeastern University
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.

Warner-Lambert
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.

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.

Northeastern University
Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands.

University of North Carolina
Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.

TBA
Combined analgesic/neuroleptic activity in N-butyrophenone prodine-like compounds.

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.

TBA
Synthesis and dopaminergic binding of 2-aryldopamine analogues: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes.

TBA
Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics.

TBA
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

Virginia Commonwealth University
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.

Friedrich-Alexander University
Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.

Friedrich-Alexander University
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.

Friedrich-Alexander University
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.

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.

University of Pisa
Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179).

Friedrich-Alexander University
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.

Friedrich-Alexander University
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.

Yale University
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.

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.

Universit£T Erlangen-N£Rnberg
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition

TBA
Dopamine autoreceptor agonists: computational studies, synthesis and biological investigations

TBA
Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385

TBA
Novel 4,5,6,7-tetrahydrobenzothiazole dopamine agonists display very low stereoselectivity in their interaction with dopamine receptors.

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.

University of Siena
First enantioselective syntheses of the dopamine D1 and D2 receptor modulators, (+)- and (-)-govadine.

University of British Columbia
Chiral indolo[3,2-f][3]benzazecine-type dopamine receptor antagonists: synthesis and activity of racemic and enantiopure derivatives.

Martin-Luther-Universit£T Halle-Wittenberg
Analogues of doxanthrine reveal differences between the dopamine D1 receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a]phenanthridines.

Quimique C£A.
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.

University of Naples Federico II
Bivalent molecular probes for dopamine D2-like receptors.

Friedrich-Alexander University
Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding.

Forschungszentrum J£Lich
Development of a bivalent dopamine D2 receptor agonist.

Friedrich-Alexander University
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.

The University of Mississippi
Assessment of dopamine D¿? receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393.

Purdue University
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.

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.

Soochow University College of Pharmaceutical Sciences
Bivalent dopamine D2 receptor ligands: synthesis and binding properties.

Friedrich-Alexander University
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists.

University of Tartu
Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.

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.

The University of Sydney
Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands.

University of Santiago De Compostela
Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions.

Friedrich-Alexander University
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands.

Chinese Academy of Sciences
Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET.

Friedrich-Alexander-UniversitäT Erlangen-NüRnberg
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.

Bristol-Myers Squibb
Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.

Friedrich-Alexander University
Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors.

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.

National Institute of Mental Health
Spiroindolones, a potent compound class for the treatment of malaria.

Swiss Tropical and Public Health Institute
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.

Purdue University
Smoothened antagonists for hair inhibition.

Pfizer
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Università
Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.

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.

Meiji Seika Kaisha
New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation.

University of Naples Federico II
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.

Friedrich-Schiller-Universit£T Jena
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.

Merck Research Laboratories
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.

Merck Research Laboratories
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.

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.

Schering-Plough Research Institute
Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

University of Naples Federico II
1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.

Friedrich-Alexander University
Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.

Novartis Institutes For Biomedical Research
Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker.

Friedrich-Alexander University
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.

Friedrich-Alexander-Universit£T
N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists.

University of Tartu
Displacement Activity of Bisbenzylisoquinoline Alkaloids at Striatal
3H-SCH 23390 and
3H-Raclopride Binding Sites

TBA
The Role of Receptor Binding in Drug Discovery

TBA
Serotonin 5-HT
4 agonist activity of a series of
meso-azanoradamantane benzamides

TBA
(E) and (Z)-3-Styrylpiperidines as sigma ligands

TBA
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)

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 D
1 antagonist (AS-300)

TBA
Novel HO-DPAT (hydroxy-2-dipropylaminotetralin) isomers: Stereoselective synthesis and receptor binding studies

TBA
Dopamine receptor binding properties of some 2,3,4,5-tetrahydro-1
H-3-benzazepine-7-ols with non-aromatic substituents in the 5-position

TBA
Synthesis and evaluation of several cathechol bioisosteres as potential dopamine receptor ligands

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).

TBA
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.

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.

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.

University of Siena
Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.

Harvard Medical School
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.

Chinese Academy of Sciences
Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.

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.

University of Michigan
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.

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.

National Institute On Drug Abuses
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.

Merck Research Laboratories
Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands.

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.

Florida A&M University
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.

Harvard Medical School
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines.

Chinese Academy of Sciences
Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines.

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.

University of Belgrade
Halogenated boldine derivatives with enhanced monoamine receptor selectivity.

Universidad De Chile
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.

Universidad De Valencia
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.

Korea Research Institute of Chemical Technology
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.

Pfizer
Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes.

Friedrich-Alexander University
In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors.

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.

Friedrich-Schiller-UniversitäT Jena
Transformation of a Dopamine D

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.

National Institute of Mental Health
Dopamine D

National Institute On Drug Abuse?Intramural Research Program
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.

Harvard Medical School
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.

Institut D'Investigacions BiomèDiques August Pi I
Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D

Kindai University
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists.

Friedrich-Alexander-Universitat Erlangen-Nurnberg
Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.

Tianjin University
Novel sigma receptor ligands: synthesis and biological profile.

University of Catania
Targeting σ

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.

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.

Friedrich-Alexander University
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.

High Point University
Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.

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.

Friedrich-Schiller-UniversitäT Jena
From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.

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.

Friedrich-Schiller-UniversitäT Jena
Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.

Schering-Plough Research Institute
Modification of the clozapine structure by parallel synthesis.

Schering-Plough Research Institute
Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists.

Friedrich-Alexander University
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Pfizer
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.

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.

Friedrich-Schiller-UniversitäT Jena
Abolishing Dopamine D

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.

Columbia University College of Physicians and Surgeons
Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists.

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.

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.

Università
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.

Columbia University College of Physicians and Surgeons
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.

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.

7Tm Pharma
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.

Università
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.

Zhejiang University
2-(Fluoromethoxy)-4'-(

Universidad Complutense De Madrid
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.

H. Lundbeck
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.

Friedrich-Alexander University
Synthesis of 3-arylpiperazinylalkylpyrrolo[3,2-d]pyrimidine-2,4-dione derivatives as novel, potent, and selective alpha1-adrenoceptor ligands.

Università
Research progress in biological activities of isochroman derivatives.

Shaanxi University of Chinese Medicine
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.

Johnson & Johnson Pharmaceutical Research & Development
Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies.

Università
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.

TBA
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y

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.

Friedrich-Schiller-UniversitäT Jena
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators.

Pfizer
Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.

University of Erlangen-Nuremberg
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.

Pfizer
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.

Wyeth Research
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D

Shanghaitech University
New tetrahydroisoquinoline-based D

City University of New York
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.

Cracow University of Technology
1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.

Neurogen
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.

Yale University
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y

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.

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.

University Center For Pharmacy
Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.

Friedrich-Alexander University
Structure-Activity Relationship of Heterocyclic P2Y

National Institute of Diabetes and Digestive and Kidney Diseases
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine D

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.

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.

Université
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.

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.

Friedrich-Alexander University
Isoquinolinone derivatives as potent CNS multi-receptor D

Jiangsu Ocean University
The Essential Medicinal Chemistry of Cannabidiol (CBD).

University of Minnesota
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.

Pharmazeutisches Institut Der UniversitäT Freiburg
Development of pyrimidone D1 dopamine receptor positive allosteric modulators.

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 D

Sumitomo Dainippon Pharma.
Dopaminergic 7-aminotetrahydroindolizines: ex-chiral pool synthesis and preferential D3 receptor binding.

Friedrich-Alexander University
Identification of C10 nitrogen-containing aporphines with dopamine D

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).

Friedrich-Alexander University
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT

City University of New York
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines.

City University of New York
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.

Columbia University College of Physicians and Surgeons
Enantioselective syntheses of dopaminergic (R)- and (S)-benzyltetrahydroisoquinolines.

Universidad De Valencia
Cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies.

University of Crete
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge

University of Mississippi
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.

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.

Astrazeneca R&D SöDertäLje
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.

University of Tokyo
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D

National Institute of Neurological Disorders and Stroke
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.

Shanghaitech University
Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.

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.

Knoll Pharmaceuticals
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D

University of Pennsylvania
2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.

UniversitäT Erlangen - NüRnberg
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D

University of North Carolina At Chapel Hill
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.

University of GöTeborg
N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.

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.

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).

Centro De InvestigacióN Grupo Ferrer
Novel Strategies To Activate the Dopamine D

Ucb Pharma
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.

Shanghaitech University
NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.

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.

Medical University of Lublin
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.

Rti International
Serotonergic ergoline derivatives.

Pharmacia & Upjohn
Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.

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 D

Temple University
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.

Duke University
Chemical synthesis, microbial transformation and biological evaluation of tetrahydroprotoberberines as dopamine D1/D2 receptor ligands.

Huzhou University
Novel Pyrazolyl-dihydroisoquinolines as Positive Allosteric Modulator of the Dopamine D1 Receptor.

Arrival Discovery
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1

Amri
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.

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 pr

Abbott Laboratories
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D

Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.

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]

Université
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT

University of Minnesota Twin Cities
11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.

Uppsala University
10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.

Uppsala University
(+/-)-3-[4'-(N,N-dimethylamino)cinnamyl]benzazepine analogs: novel dopamine D1 receptor antagonists.

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.

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.

Yamanouchi Pharmaceutical
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.

Pharmacia & Upjohn
Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping.

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.

Hoechst-Roussel Pharmaceuticals
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.

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.

University of Lund
3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.

Eli Lilly
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.

Virginia Commonwealth University
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar
New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study.

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.

Vanderbilt University
2,3,9- and 2,3,11-trisubstituted tetrahydroprotoberberines as D2 dopaminergic ligands.

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.

University of North Carolina
3,4-Dihydroxy- and 3,4-methylenedioxy- phenanthrene-type alkaloids with high selectivity for D2 dopamine receptor.

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.

Parke-Davis Pharmaceutical Research
Dopaminergic benzo[a]phenanthridines: resolution and pharmacological evaluation of the enantiomers of dihydrexidine, the full efficacy D1 dopamine receptor agonist.

Purdue University
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.

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.

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.

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.

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-phenyldopamin

Purdue University
Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.

H. Lundbeck
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.

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.

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.

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.

Universidad De Santiago
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.

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.

Sandoz Pharma
Synthesis and atypical antipsychotic profile of some 2-(2-piperidinoethyl)benzocycloalkanones as analogues of butyrophenone.

University of Santiago De Compostela
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.

Glaxo Research and Development
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.

Huazhong University of Science and Technology
New Dopamine D3-Selective Receptor Ligands Containing a 6-Methoxy-1,2,3,4-tetrahydroisoquinolin-7-ol Motif.

City University of New York
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.

Pfizer
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.

Texas Tech University Health Sciences Center
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.

Northeastern University
Synthesis of 3-(3-hydroxyphenyl)pyrrolidine dopamine D

Southern Illinois University Edwardsville
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y

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.

TBA
Substituted benzamides with conformationally restricted side chains. 2. Indolizidine derivatives as central dopamine receptor antagonists.

Beecham Pharmaceuticals Research Division
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.

Warner-Lambert
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents.

Warner-Lambert/Parke-Davis Pharmaceutical Research
New 5-HT

Dipartimento Di Farmacia Universit£
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.

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.

Schering-Plough
Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

Vanderbilt University
Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.

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.

University of Pennsylvania
Aporphines as antagonists of dopamine D-1 receptors.

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.

Research Biochemicals
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.

Janssen Infectious Diseases-Diagnostics
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.

Phenex Pharmaceuticals
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.

Research Biochemicals
Development of molecular tools based on the dopamine D

Friedrich-Alexander University
Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues.

Northeastern University
Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

Vanderbilt University
β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.

Friedrich-Alexander University Erlangen-N£Rnberg
Return of D

University of Nebraska Medical Center
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.

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.

H. Lundbeck
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.

Harvard Medical School
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.

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.

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.

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.

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.

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.

Hoechst-Roussel Pharmaceuticals
Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds forβ-Arrestin-Biased D

Friedrich-Alexander University Erlangen-Nuernberg
RNA virus inhibitor compounds and uses thereof

University of Alberta
NOVEL COMPOUNDS

Sitryx Therapeutics
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION

Genentech
MACROCYCLIC PEPTIDOMIMETIC PROTEASE INHIBITOR AND USE THEREOF

Tencent Technology (Shenzhen)
Indazole carboxamides as kinase inhibitors

Bristol-Myers Squibb
SELECTIVE MODULATORS OF ATAXIA TELANGIECTASIA MUTATED (ATM) KINASE AND USES THEREOF

Suzhou Zanrong Pharma
COMPOUND AS BRAIN-PERMEABLE BTK OR HER2 INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF

Chengdu Hyperway Pharmaceuticals
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes

Sprint Bioscience
LDHA activity inhibitors

Arctic Pharma
N-((HET)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors

Kalvista Pharmaceuticals
Compounds as rearranged during transfection (RET) inhibitors

Glaxosmithkline Intellectual Property Development
Indane-amines as PD-L1 antagonists

Chemocentryx
Heterocyclic inhibitors of monocarboxylate transporter

The Scripps Research Institute
Ethyldiamine orexin receptor antagonists

Merck Sharp & Dohme
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

Ctxt
Methods of use of cyclopamine analogs

Infinity Pharmaceuticals
Inhibitors of PTP4A3 for the treatment of cancer

University of Virginia Patent Foundation
Compounds and compositions for inhibiting the activity of SHP2

Novartis
Tricyclic heterocyclic compounds useful as inhibitors of TNF

Bristol-Myers Squibb
Fucosidase inhibitors

Horizon Orphan
Therapeutic compounds and compositions, and methods of use thereof

Genentech
Pyridinyl and fused pyridinyl triazolone derivatives

Takeda Pharmaceutical
Compounds for the inhibition of cyclophilins and uses thereof

Merck Patent
Heteroaromatic compounds as BTK inhibitors

Boehringer Ingelheim International
Urea and amide derivatives of aminoalkylpiperazines and use thereof

Southern Research Institute
Morphinan derivative

University of Tsukuba
Pyrrolopyrimidine compound or salt thereof and compositions containing the pyrrolopyrimidine compound or salt thereof

Taiho Pharmaceutical
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives

Idorsia Pharmaceuticals
Styryl quinazoline derivatives as pharmaceutically active agents

Vichem Chemie Kutató
Oxazoline and isoxazoline derivatives as CRAC modulators

Lupin
Compounds as rearranged during transfection (RET) inhibitors

Glaxosmithkline
C-ring modified tricyclic benzonaphthiridinone protein kinase inhibitors and use thereof

Merck Patent
Isoquinolin-3-yl carboxamides and preparation and use thereof

Samumed
Morphan and morphinan analogues, and methods of use

Alkermes Pharma Ireland
Pyridazinone compounds and their use as DAAO inhibitors

Takeda Pharmaceutical
Syk inhibitors

Gilead Sciences
Salt of fused pyrimidine compound and crystal thereof

Taiho Pharmaceutical
Inhibitors of plasma kallikrein

Kalvista Pharmaceuticals
Non-annulated thiophenylamides

Hoffmann-La Roche
Synthesis and biological activity of progesterone derivatives as 5alpha-reductase inhibitors, and their effect on hamster prostate weight.

Universidad Nacional Autonoma De Mexico
Phosphonate derivatives and methods of use thereof in the treatment of Alzheimer's disease

University of Kansas
Structural determinants of Tau aggregation inhibitor potency.

The Ohio State University
1,3,5-triazine-2-amine derivatives, preparation thereof and diagnostic and therapeutic use thereof

Sanofi
5-alkynyl-pyridines

Boehringer Ingelheim International
Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors.

University of Karachi
Chymase inhibitors

Boehringer Ingelheim International
Pyrazolopyrimidines Establish MurC as a Vulnerable Target in Pseudomonas aeruginosa and Escherichia coli.

Astrazeneca India
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes

Merck Sharpe & Dohme
Inhibition of AcpA phosphatase activity with ascorbate attenuates Francisella tularensis intramacrophage survival.

University of Florida
Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel.

National Cancer Institute-Frederick
SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation.

Sanofi-Synthelabo Research
Novel cyclic peptide agonist of high potency and selectivity for the type II vasoactive intestinal peptide receptor.

University of California San Francisco
The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase.

Vertex Pharmaceuticals
DcpS as a therapeutic target for spinal muscular atrophy.

Decode Chemistry
A new screening assay for allosteric inhibitors of cSrc.

Chemical Genomics Centre of The Max Planck Society
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.

The Scripps Research Institute
Identification of RIP1 kinase as a specific cellular target of necrostatins.

Tufts University
Splicing factor SF3b as a target of the antitumor natural product pladienolide.

Eisai
Correlating solution binding and ESI-MS stabilities by incorporating solvation effects in a confined cucurbit[8]uril system.

University of Cambridge
Calorimetric Studies on the Complexation of Several Ferrocene Derivatives by .alpha.- and .beta.-Cyclodextrin. Effects of Urea on the Thermodynamic Parameters

University of Miami
Chiral Recognition Thermodynamics of β-Cyclodextrin: The Thermodynamic Origin of Enantioselectivity and the Enthalpy-Entropy Compensation Effect

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.

Virginia Commonwealth University
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.

Ono Pharmaceutical
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.

Vernalis (R&D)
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.

Wyeth Research
Biarylether amide quinolines as liver X receptor agonists.

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.

Duquesne University
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases.

University of Alabama At Birmingham
Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.

Cnrs
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

Johnson & Johnson Pharmaceutical
Compounds binding to the S2-S3 pockets of thrombin.

University of Kalmar
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Bristol-Myers Squibb
Chalcones: a valid scaffold for monoamine oxidases inhibitors.

Sapienza University of Rome
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.

Universita Del Piemonte Orientale
Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.

Bristol-Myers Squibb
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

Wyeth Research
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.

Absolute Science
1-Sulfonylindazoles as potent and selective 5-HT6 ligands.

Wyeth Research
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.

Nerviano Medical Sciences
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.

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.

Abbott Laboratories
Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.

Schering-Plough Research Institute
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.

Valeant Pharmaceuticals Research and Development
Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors.

University of Southern California
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.

Burnham Institute For Medical Research
The molecular interactions of buspirone analogues with the serotonin transporter.

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).

Saarland University
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.

Sunesis Pharmaceuticals
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.

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.

Purdue University
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.

Astrazeneca
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo.

Irbm/Merck Research Laboratories
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.

Novartis
Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase.

Bryn Mawr College
Structure of the BH3 domains from the p53-inducible BH3-only proteins Noxa and Puma in complex with Mcl-1.

University of Otago