505 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Virginia Commonwealth University
(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/s
University of Catania
Norbenzomorphan Scaffold: Chemical Tool for Modulating Sigma Receptor-Subtype Selectivity.
The University of Texas At Austin
Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.
University of Pavia
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Gaining in pan-affinity towards sigma 1 and sigma 2 receptors. SAR studies on arylalkylamines.
University of Pavia
Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.
National Institute On Drug Abuse
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.
Icahn School of Medicine At Mount Sinai
Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
University of Trieste
Oxa-Pictet-Spengler reaction as key step in the synthesis of novels receptor ligands with 2-benzopyran structure.
Universit£T M£Nster
Rigidity versus Flexibility: Is This an Issue ins1 Receptor Ligand Affinity and Activity?
University of M£Nster
One-pot synthesis and sigma receptor binding studies of novel spirocyclic-2,6-diketopiperazine derivatives.
University of Tehran
Synthesis and Biological Evaluation of Novels1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.
Huazhong University of Science and Technology
Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as sigma-1 (s1) receptor antagonists for the treatment of pain.
Renmin Hospital of Wuhan University
Tetrahydroprotoberberine alkaloids with dopamine ands receptor affinity.
City University of New York
Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.
Modena and Reggio Emilia
Development of sigma-1 (s1) receptor fluorescent ligands as versatile tools to studys1 receptors.
University of Bari Aldo Moro
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists ors1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
University of Camerino
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.
Washington University
New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
Institute of Radiopharmaceutical Cancer Research
Novel 1-(2-aryl-2-adamantyl)piperazine derivatives with antiproliferative activity.
University of Athens
Synthesis and structure-activity relationship study of a new series of selectives(1) receptor ligands for the treatment of pain: 4-aminotriazoles.
Esteve
Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
University of Lille
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.
Northwestern University
Synthesis and evaluation of tetrahydroindazole derivatives as sigma-2 receptor ligands.
Guangdong Medical College
Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
University of Trieste
Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
D'Annunzio University of Chieti���Pescara
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted¿-opioid receptor agonists.
Westf£Lische Wilhelms-Universit£T M£Nster
Pyridine analogues of spirocyclics1 receptor ligands.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
Ether modifications to 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (SA4503): effects on binding affinity and selectivity for sigma receptors and monoamine transporters.
University of Missouri
Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity froms2 receptor affinity in mixed P-gp/s2 receptor agents.
University of Bari Aldo Moro
From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.
University of Bari Aldo Moro
Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.
University of Lille
Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain.
Huazhong University of Science and Technology
Identification, pharmacological evaluation and binding mode analysis of novel chromene and chromane baseds1 receptor ligands.
University of Trieste
Combination of cyclohexane and piperazine based¿-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues ass2 receptor ligands.
Washington University
Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent ands receptors binding properties.
University of Bari Aldo Moro
Synthesis, pharmacological evaluation, ands1 receptor interaction analysis of hydroxyethyl substituted piperazines.
University of M£Nster
Thes2 receptor: a novel protein for the imaging and treatment of cancer.
Washington University
Synthesis and biological evaluation of a novel sigma-1 receptor antagonist based on 3,4-dihydro-2(1H)-quinolinone scaffold as a potential analgesic.
Huazhong University of Science and Technology
Molecular similarity, quantitative chirality, and QSAR for chiral drugs.
University of Oxford
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
University of Missouri
Involvement of apoptosis and autophagy in the death of RPMI 8226 multiple myeloma cells by two enantiomeric sigma receptor ligands.
University of Greifswald
Structure of thes1 receptor and its ligand binding site.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
From NMDA receptor antagonists to discovery of selectives2 receptor ligands.
University of Messina
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
National Institute of Mental Health
Design, synthesis and receptor affinity of novel conformationally restricteds ligands based on the [4.3.3]propellane scaffold.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.
University of Bari Aldo Moro
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Glaxosmithkline
Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging ofs2 receptors.
University of Bari Aldo Moro
New combination of pharmacophoric elements of potents1 ligands: design, synthesis ands receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
Universit£T M£Nster
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.
Virginia Commonwealth University
Discovery of ML314, a Brain Penetrant Non-Peptidicβ-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Sanford-Burnham Medical Research Institute
Structure activity relationship study of benzo[d]thiazol-2(3H)one baseds receptor ligands.
University of Mississippi
Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates.
Columbia University Medical Center
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.
Washington University
Synthesis and receptor binding studies of novel 4,4-disubstituted arylalkyl/arylalkylsulfonyl piperazine and piperidine-based derivatives as a new class ofs1 ligands.
Nstri
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Ucl School of Pharmacy
Synthesis and biological evaluation of Esaprazole analogues showings1 binding and neuroprotective properties in vitro.
Nensius Research
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
Institute of Organic Synthesis
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
Broad Institute of Mit and Harvard
Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives ass1 receptor ligands for positron emission tomography imaging.
Key Laboratory of Radiopharmaceuticals Beijing Normal University
Improvement ofs1 receptor affinity by late-stage C-H-bond arylation of spirocyclic lactones.
Wilhelms-Universit£T M£Nster
Investigation ofs receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
University of Bari Aldo Moro
Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selectives1 receptor ligands.
Esteve
3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (s1) receptor.
Northeast Ohio Medical University
Design and synthesis of new bifunctional sigma-1 selective ligands with antioxidant activity.
University of Catania
Synthesis and biological evaluation of¹8F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
Key Laboratory of Radiopharmaceuticals (Beijing Normal University)
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.
University of North Carolina
Spiropiperidines as high-affinity, selective sigma ligands.
Merck Sharp and Dohme Research Laboratories
Benz[f]isoquinoline analogues as high-affinity sigma ligands.
Merck Sharp and Dohme Research Laboratories
Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.
University of Camerino
Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines.
University of Lausanne
New adamantane phenylalkylamines withs-receptor binding affinity and anticancer activity, associated with putative antagonism of neuropathic pain.
National and Kapodistrian University of Athens
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.
Savannah State 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
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
TBA
New positron emission tomography (PET) radioligand for imagings-1 receptors in living subjects.
Stanford University
Enantiomerically pure 1,3-dioxanes as highly selective NMDA ands1 receptor ligands.
Westf£Lische Wilhelms-Universit£T M£Nster
Pd-catalyzed direct C-H bond functionalization of spirocyclics1 ligands: generation of a pharmacophore model and analysis of the reverse binding mode by docking into a 3D homology model of thes1 receptor.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Esteve
Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents.
Sk Biopharmaceuticals
Exploration of ring size in a series of cyclic vicinal diamines withs1 receptor affinity.
The University of Sydney
Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
Kanazawa University
Thiophene bioisosteres of spirocyclics receptor ligands: relationships between substitution pattern ands receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Washington University
Microwave assisted synthesis of spirocyclic pyrrolidines -s1 receptor ligands with modified benzene-N-distance.
Institut F£R Pharmazeutische Und Medizinische Chemie
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.
The University of Sydney
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Synthesis,s1,s2-receptors binding affinity and antiproliferative action of new C1-substituted adamantanes.
National and Kapodistrian University of Athens
Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with highs1 receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Arylamides hybrids of two high-affinitys2 receptor ligands as tools for the development of PET radiotracers.
University of Bari Aldo Moro
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
Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626.
Washington University
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Wilhelms-Universit£T M£Nster
Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
University of Minnesota
Synthesis of sigma receptor ligands with unsymmetrical spiro connection of the piperidine moiety.
Institut F£R Pharmazeutische Und Medizinische Chemie
Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).
Universita Degli Studi Di Bari
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
University of Trieste
Relationships between the structure of 6-substituted 6,8-diazabicyclo[3.2.2]nonan-2-ones and their sigma receptor affinity and cytotoxic activity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
National Institute On Drug Abuse-Intramural Research Program
Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.
Universita Degli Studi Di Bari
Synthesis and structure-affinity relationships of novel spirocyclic sigma receptor ligands with furopyrazole structure.
Westf£Lische Wilhelms-Universit£T M£Nster
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
The University of Mississippi
PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma.
University of Bari Aldo Moro
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
University of Bari Aldo Moro
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Synthesis and structure-activity relationships of N-(3-phenylpropyl)-N'-benzylpiperazines: Potent ligands for sigma1 and sigma2 receptors.
University of Missouri-Columbia
Synthesis of bicyclic sigma receptor ligands with cytotoxic activity.
University M£Nster
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
University of Bari Aldo Moro
Synthesis of bridged piperazines with sigma receptor affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
Ono Pharmaceutical
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
University of Bari Aldo Moro
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
University of Innsbruck
Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands.
University of Modena and Reggio Emilia
Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.
Nida-Irp
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
University of Bari Aldo Moro
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
Pharmazeutisches Institut Der Universit£T Freiburg
Synthesis of (+)-cis-N-(4-isothiocyanatobenzyl)-N-normetazocine, an isothiocyanate derivative of N-benzylnormetazocine as acylant agent for the sigma(1) receptor.
University of Catania
Current and novel approaches to the drug treatment of schizophrenia.
Merck Sharp and Dohme Research Laboratories
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
Otsuka Pharmaceutical
Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs.
Taisho Pharmaceutical
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Warner-Lambert
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.
Taisho Pharmaceutical
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors.
University of Illinois At Chicago
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
National Taiwan University
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.
Astra Arcus
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.
University of Catania
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
Cooperation Pharmaceutique Fran�Aise
Isothiocyanate derivatives of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole): irreversible ligands for the dopamine transporter.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.
Cambridge Neuroscience
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
National Institute of Diabetes and Digestive and Kidney Diseases
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
University of Bari Aldo Moro
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
Synthesis and sigma binding properties of 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans.
Research Triangle Institute
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.
H. Lundbeck
Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.
H. Lundbeck
Antipodal alpha-N-(methyl through decyl)-N-normetazocines (5,9 alpha-dimethyl-2'-hydroxy-6,7-benzomorphans): in vitro and in vivo properties.
Virginia Commonwealth University
A new approach to the design of sigma-2-selective ligands: synthesis and evaluation of N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine-related polyamines at sigma-1 and sigma-2 receptor subtypes.
National Institutes of Diabetes and Digestive and Kidney Diseases
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.
National Institute On Drug Abuse-Intramural Research Program
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Albany Molecular Research
Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and binding characteristics of potential SPECT imaging agents for sigma-1 and sigma-2 binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Synthesis and evaluation of conformationally restricted N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamines at sigma receptors. 2. Piperazines, bicyclic amines, bridged bicyclic amines, and miscellaneous compounds.
National Institute of Diabetes and Digestive and Kidney Diseases
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
National Institute On Drug Abuse
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
Novel piperidine sigma receptor ligands as potential antipsychotic drugs.
Dupont Pharmaceuticals
Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.
National Institute of Diabetes and Digestive and Kidney Diseases
Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.
Virginia Commonwealth University
Identification and exploitation of the sigma-opiate pharmacophore.
Virginia Commonwealth University
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
Hoechst-Roussel Pharmaceuticals
Synthesis and structure-activity relationships of N,N'-di-o-tolylguanidine analogues, high-affinity ligands for the haloperidol-sensitive sigma receptor.
University of Oregon
Synthesis and evaluation of N-substituted cis-N-methyl-2-(1-pyrrolidinyl)cyclohexylamines as high affinity sigma receptor ligands. Identification of a new class of highly potent and selective sigma receptor probes.
National Institute of Diabetes and Digestive and Kidney Diseases
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Pfizer
Benzofuro[2,3-c]pyridin-6-ols: synthesis, affinity for opioid-receptor subtypes, and antinociceptive activity.
Ciba-Geigy
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
National Institute of Digestive
Phencyclidine-like effects of tetrahydroisoquinolines and related compounds.
G. D. Searle
N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors.
University of G£Teborg
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Ucb Pharma
Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.
Pharmacia & Upjohn
Trishomocubanes, a new class of selective and high affinity ligands for the sigma binding site
TBA
(5S)-3-aryl-5-(1-piperidinylmethyl)-2-oxazolidinones, a new class of potential neuroleptics with a high affinity for sigma receptors
TBA
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
Institute of Radiopharmacy
Synthesis and biological characterization of 3-substituted-1H-indoles as ligands of GluN2B-containing N-methyl-D-aspartate receptors.
University of Messina
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities ass¿? receptor ligands.
University of Bari Aldo Moro
Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand.
University of Wisconsin School of Medicine and Public Health
Identification of a potent and selectives¿? receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells.
University of Pavia
Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novels1 receptor PET imaging agent.
The University of Sydney
Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazines¿? receptor ligands.
The University of Sydney
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
The University of Mississippi
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University of Sydney
Fluorescent derivatives ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.
Universita` Degli Studi Di Bari Aldo Moro
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.
Washington University
Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound.
Washington University
Synthesis of 7,9-diazabicyclo[4.2.2]decanes as conformationally restricted κ receptor agonists: fine tuning of the dihedral angle of the ethylenediamine pharmacophore.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA ands receptor antagonists.
Westf£Lischen Wilhelms-Universit£T M£Nster
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
Design, synthesis and pharmacological evaluation of spirocyclics(1) receptor ligands with exocyclic amino moiety (increased distance 1).
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
Key Laboratory of Radiopharmaceuticals (Beijing Normal University)
Novel potent and selectives ligands: evaluation of their agonist and antagonist properties.
University of Catania
Synthesis and pharmacological evaluation of fluorine-containing D3 dopamine receptor ligands.
Washington University
Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for bindings1 ands2 receptors.
University of Missouri-Columbia
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Glaxosmithkline
Analogues ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
Universita` Degli Studi Di Bari Aldo Moro
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
University of Catania
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.
The University of Sydney
Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
3D QSAR study, synthesis, and in vitro evaluation of (+)-5-FBVM as potential PET radioligand for the vesicular acetylcholine transporter (VAChT).
University of Tours
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
Synthesis and resolution of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: new sigma receptor ligands with neuroprotective effect.
University of Catania
Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands.
University of Sydney
5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis and characterization of N,N-dialkyl and N-alkyl-N-aralkyl fenpropimorph-derived compounds as high affinity ligands for sigma receptors.
University of Wisconsin School of Medicine and Public Health
Synthesis and NMDA receptor affinity of fluorinated dioxadrol analogues.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhems-Universit£T M£Nster
The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.
University of Maryland
Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).
University of Pavia
Oxo-bridged isomers of aza-trishomocubane sigma (sigma) receptor ligands: Synthesis, in vitro binding, and molecular modeling.
University of Sydney
Synthesis and opioid activity of enantiomeric N-substituted 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolines.
National Taiwan University
Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
Washington University
An aromatic moiety is not essential for pharmacophore binding to sigma binding sites: Synthesis of N-alkylazacycloheptane derivatives as potent sigma ligands
TBA
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents
TBA
Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability.
Institut FüR Pharmazeutische Und Medizinische Chemie Der UniversitäT MüNster
Dancing of the second aromatic residue around the 6,8-diazabicyclo[3.2.2]nonane framework: influence on sigma receptor affinity and cytotoxicity.
Institut Fur Pharmazeutische Und Medizinische Chemie Der Westfalischen Wilhelms-Universitat Munster
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
Washington University
Relationships between the structure of 6-allyl-6,8-diazabicyclo[3.2.2]nonane derivatives and their sigma receptor affinity and cytotoxic activity.
Institut FüR Pharmazeutische Und Medizinische Chemie Der WestfäLischen Wilhelms-UniversitäT MüNster
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Merck Research Laboratories
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
Institut FüR Pharmazeutische and Medizinische Chemie Der UniversitäT MüüNster
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
National Institute of Mental Health
1,4-Diazepanes derived from (S)-serine--homopiperazines with improved sigma(1) (sigma) receptor affinity and selectivity.
Institut FüR Pharmazeutische Und Medizinische Chemie
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
University of Maryland
Substituted benzo[d]oxazol-2(3H)-one derivatives with preference for the sigma1 binding site.
University of Trieste
Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.
University of Trieste
Nitrile analogs of meperidine as high affinity and selective sigma-1 receptor ligands.
University of Maryland
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
National Institute of Diabetes and Digestive and Kidney Disease
Synthesis and evaluation of novel radioiodinated benzamides for malignant melanoma.
Radiopharmaceuticals Research Institute
Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.
Washington 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
Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
University Munster
2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance.
Xuzhou Medical University
2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design.
Shanghaitech University
Synthesis and in vitro evaluation of tetrahydroisoquinolinyl benzamides as ligands for sigma receptors.
University of Missouri-Columbia
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents.
University of Pavia
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity.
University of Messina
Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.
Universit£
What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
University of Illinois At Chicago
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
Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.
University of Catania
From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.
University of Nebraska Medical Center
Bitopic Sigma 1 Receptor Modulators to Shed Light on Molecular Mechanisms Underpinning Ligand Binding and Receptor Oligomerization.
University of Pavia
The Emerging Landscape of Small-Molecule Therapeutics for the Treatment of Huntington's Disease.
Aligarh Muslim University
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Recent advancements in chromone as a privileged scaffold towards the development of small molecules for neurodegenerative therapeutics.
Jamia Millia Islamia
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
University of Texas At Austin
Synthesis of 8-aminomorphans with high KOR affinity.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
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
11C-labeling of n-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]arylcarboxamide derivatives and evaluation as potential radioligands for PET imaging of dopamine D3 receptors.
University of Milano/Bicocca
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
Université
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.
Université
Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
University of Catania
Synthesis and biological evaluation of conformationally restricted GluN2B ligands derived from eliprodil.
Westf£Lische Wilhelms-Universit£T M£Nster
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.
Yeditepe University
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
University of Trieste
Research progress in biological activities of isochroman derivatives.
Shaanxi University of Chinese Medicine
Benzylaminofentanyl derivates: Discovery of bifunctional μ opioid and σ
Jiangsu Ocean University
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
Beijing Normal University
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.
Kanazawa University
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ
University of Bari Aldo Moro
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability.
The University of Kansas
Optimization of bifunctional piperidinamide derivatives as σ
Huazhong University of Science and Technology
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ
Esteve Pharmaceuticals
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
Università
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Virginia Commonwealth University
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M
Vanderbilt University
Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Wake Forest University School of Medicine
Chemoenzymatic synthesis of 2,6-disubstituted tetrahydropyrans with high σ
Westf£Lische Wilhelms-Universit£T M£Nster
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.
The State University of New Jersey
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.
Huazhong University of Science and Technology
Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σ
Guangdong Medical University
Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.
Università
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Soochow University
New bifunctional antioxidant/σ1 agonist ligands: Preliminary chemico-physical and biological evaluation.
University of Catania
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
Westf£Lische Wilhelms-Universit£T M£Nster
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
National Institute On Drug Abuse - Intramural Research Program
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.
Université
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
University of Catania
N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.
University of Maryland
Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer's Disease.
Usona Institute
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1.
Pharmazeutisches Institut Der UniversitäT Freiburg
Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.
Universit£T M£Nster
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
Wake Forest University School of Medicine
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu
Vanderbilt University
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
Wake Forest University School of Medicine
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents.
University of Modena and Reggio Emilia
Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation.
University of Catania
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.
University of Trieste
Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.
National Institute On Drug Abuse-Intramural Research Program
Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues.
Virginia Commonwealth University
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.
Westf£Lische Wilhelms-Universit£T M£Nster
Radioiodinated N-(2-diethylaminoethyl)benzamide derivatives with high melanoma uptake: structure-affinity relationships, metabolic fate, and intracellular localization.
University of Heidelberg
Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.
East China Normal University
Synthesis of spiro-2,6-dioxopiperazine and spiro-2,6-dioxopyrazine scaffolds using amino acids in a three-component reaction to generate potential Sigma-1 (σ
Memorial Sloan Kettering Cancer Center
A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.
University of Maryland
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.
Research Triangle Institute
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College of Wisconsin
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Synthesis, in vitro and in vivo characterization of new benzoxazole and benzothiazole-based sigma receptor ligands.
University of Catania
Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
University of Minnesota
Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands.
Northwestern University
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
Florida A&M University
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D
University of North Carolina At Chapel Hill
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety.
Universit£T M£Nster
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
Development of Novel Quinoxaline-Based κ-Opioid Receptor Agonists for the Treatment of Neuroinflammation.
Universit£T M£Nster
Combinatorial chemistry: from peptides and peptidomimetics to small organic and heterocyclic compounds.
Institute For Molecular Studies
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ
Esteve Pharmaceuticals
Characterization of novel N,N'-disubstituted piperazines as sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands.
Università
Indole: A privileged scaffold for the design of anti-cancer agents.
Hunan University of Science and Technology
Substituted halogenated arylsulfonamides: a new class of sigma receptor binding tumor imaging agents.
The George Washington University Medical Center
Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
Wake Forest University School of Medicine
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
University of Camerino
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
University of Louvain
N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
University of Minnesota
Halogenated 4-(phenoxymethyl)piperidines as potential radiolabeled probes for sigma-1 receptors: in vivo evaluation of [123I]-1-(iodopropen-2-yl)-4-[(4-cyanophenoxy)methyl]pip eri dine.
Ansto
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.
University of Trieste
Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.
University Munster
Synthesis and in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site.
Scios Nova
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencyclidine binding site.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and structure-activity studies of N,N'-diarylguanidine derivatives. N-(1-naphthyl)-N'-(3-ethylphenyl)-N'-methylguanidine: a new, selective noncompetitive NMDA receptor antagonist.
Cambridge Neuroscience
Synthesis and receptor binding studies of some new arylcarboxamide derivatives as sigma-1 ligands.
University of Trieste
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
University of GöTeborg
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
University of Maryland
Structural features important for sigma 1 receptor binding.
Virginia Commonwealth University
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.
George Washington University Medical Center
Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.
University of Maryland
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.
University of Pennsylvania
Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Smithkline Beecham Farmaceutici
A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
National Taiwan 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
Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors.
Warner-Lambert
N-(1-arylpropionyl)-4-aryltetrahydropyridines, a new class of high-affinity selective sigma receptor ligands.
New York University
(+)-cis-N-(para-, meta-, and ortho-substituted benzyl)-N-normetazocines: synthesis and binding affinity at the [3H]-(+)-pentazocine-labeled (sigma 1) site and quantitative structure-affinity relationship studies.
Research Triangle Institute
Preparation of 18F-labeled muscarinic agonist with M2 selectivity.
National Institutes of Health
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
Università
Synthesis and sigma binding properties of 1'- and 3'-halo- and 1',3'-dihalo-N-normetazocine analogues.
Research Triangle Institute
(E)-8-benzylidene derivatives of 2-methyl-5-(3-hydroxyphenyl)morphans: highly selective ligands for the sigma 2 receptor subtype.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Huazhong University of Science and Technology
Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.
IQM-CSIC
Identification of dual Sigma1 receptor modulators/acetylcholinesterase inhibitors with antioxidant and neurotrophic properties, as neuroprotective agents.
University of Pavia
New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation.
University of Trieste
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Csir-National Chemical Laboratory
Synthesis of 3-aza[4.4.3]propellanes with high σ
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.
Mazandaran University of Medical Sciences
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.
Universit£T M£Nster
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.
Guangdong Medical University
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile.
Iqog, Csic
Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 protein ligands.
Universities of Lille
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
University of Camerino
β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.
Friedrich-Alexander University Erlangen-N£Rnberg
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
Universit£T M£Nster
Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novelσ
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Do spiroindolines have the potential to replace vesamicol as lead compound for the development of radioligands targeting the vesicular acetylcholine transporter?
Helmholtz-Zentrum Dresden-Rossendorf
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis of conformationally restricted 1,3-dioxanes to analyze the bioactive conformation of 1,3-dioxane-basedσ
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.
Pfizer
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
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines.
Institutions
Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pureσ ligands with 2-benzopyran structure.
Universit£T M£Nster
(+)-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
Synthesis, configuration, and activity of isomeric 2-phenyl-2-(N-piperidinyl)bicyclo[3.1.0]hexanes at phencyclidine and sigma binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and biological evaluation of conformationally restricted 2-(1-pyrrolidinyl)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methylethylenediam ines as sigma receptor ligands. 1. Pyrrolidine, piperidine, homopiperidine, and tetrahydroisoquinoline classes.
National Institute of Diabetes and Digestive and Kidney Diseases
Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.
University of Catania
Reevaluation of fenpropimorph as aσ receptor ligand: Structure-affinity relationship studies at humanσ
Virginia Commonwealth University
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.
Drexel University College of Medicine
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: structural requirements and binding affinity at the sigma receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
SPIROCYCLIC MODULATORS OF CHOLESTEROL BIOSYNTHESIS AND THEIR USE FOR PROMOTING REMYELINATION
Genentech
CONFORMATIONALLY-CONSTRAINED INHIBITORS OF 3C OR 3C-LIKE PROTEASES
Kansas State University Research Foundation
N-AROMATIC AMIDE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
Shenzhen Edk Pharmaceutical Technology
BRD4-kinase inhibitors as cancer therapeutics
H. Lee Moffitt Cancer Center and Research Institute
Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
Merck Sharp & Dohme
Use of physiological cooling active ingredients, and agents containing such active ingredients
Symrise
Substituted perhydropyrrolo[3,4-c]pyrrole derivatives and the use of same
Bayer Pharma Aktiengesellschaft
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
Substituted pyrimidines containing acidic groups as TLR7 modulators
Apros Therapeutics
Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide.
Sakarya University
Oxazetidine derivatives, process for preparing them and use in human medicine and in cosmetics
Galderma Research & Development
Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases.
Universit�� Degli Studi Di Siena
Highly Potent Cell-Permeable and Impermeable NanoLuc Luciferase Inhibitors.
Promega Biosciences
Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
Merck Sharp & Dohme
Inhibition of WDR5 interaction with its binding partners
The Regents of The University of Michigan
Heterocyclic compounds for the treatment of stress-related conditions
Otsuka Pharmaceutical
N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer
Korea Research Institute of Chemical Technology
Substituted 7-azabicyles and their use as orexin receptor modulators
Janssen Pharmaceutica
Complexation and chiral recognition thermodynamics of 6-amino-6-deoxy-beta-cyclodextrin with anionic, cationic, and neutral chiral guests: counterbalance between van der Waals and coulombic interactions.
Japan Science and Technology Agency
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
Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase.
Almirall
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
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
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.
Nerviano Medical Sciences
2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocket.
Boehringer Ingelheim Pharmaceuticals
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease.
Neurocrine Bioscience
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
Harvard Medical School
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Sunesis Pharmaceuticals