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244 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27997171 48 Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.EBI The University of Newcastle
1732545 27 Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.EBI University of Uppsala
1995893 81 Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships.EBI Ferrosan A/S
2299626 18 Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.EBI University of Uppsala
2258904 21 Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.EBI Uppsala University
3346873 24 Derivatives of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.EBI University of Uppsala
3336015 8 Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.EBI University of California
3572973 1 Kinetics of solvolysis and muscarinic actions of an N-methyl-N-(2-bromoethyl)amino analogue of oxotremorine.EBI TBA
3494849 3 6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.EBI TBA
12113806 40 Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.EBI Ghent University
11354386 90 Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.EBI University of Mainz
27876250 60 Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHEBI Jagiellonian University Medical College
27939174 84 Challenges in the development of an MEBI Vanderbilt University Medical Center
27839919 192 Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI University of Kansas
27564135 499 1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.EBI Aptuit s.r.l
27185330 60 Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.EBI Vanderbilt University Medical Center
26988801 55 Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.EBI Jagiellonian University Medical College
26951894 376 1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.EBI Aptuit s.r.l
26786693 153 Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI Aptuit s.r.l
26516782 59 Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.EBI University of Copenhagen
26494260 36 Muscarinic acetylcholine receptor binding affinities of pethidine analogs.EBI University of Kentucky
26471092 23 Molecular hybridization yields triazole bronchodilators for the treatment of COPD.EBI Pfizer Inc
26299349 66 Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.EBI Eli Lilly and Company
25629394 52 Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist..EBI Theravance Biopharma, Inc.
25800115 62 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.EBI Rhône-Poulenc Rorer
24980056 44 Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.EBI Universit£ di Camerino
25275964 171 Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).EBI Universit£ di Camerino
25147929 105 Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).EBI Vanderbilt University Medical Center
24844758 6 Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.EBI Keio University
24805037 380 Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI Adamed Ltd.
24690494 92 Antagonists of the kappa opioid receptor.EBI The Scripps Research Institute
18077164 40 Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.EBI Universit£ di Camerino
23379472 187 Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.EBI University of Arkansas for Medical Sciences
23200253 67 Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.EBI Vanderbilt University Medical Center
23177787 59 Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.EBI Vanderbilt University Medical Center
22047691 76 The discovery of AZD9164, a novel muscarinic M3 antagonist.EBI AstraZeneca
21036043 78 The discovery of new spirocyclic muscarinic M3 antagonists.EBI AstraZeneca
20709550 80 The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.EBI GlaxoSmithKline
20483611 89 2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.EBI GlaxoSmithKline
20483599 81 2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.EBI GlaxoSmithKline
19896386 85 Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.EBI Universit£ di Camerino
19928767 88 Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.EBI Universita di Firenze
19243945 73 M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.EBI GlaxoSmithKline
18818072 162 Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.EBI GlaxoSmithKline
18798607 27 Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
18543900 105 Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.EBI Universit£ di Firenze
18680280 34 Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
18595721 32 Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.EBI Alma Mater Studiorum-University of Bologna
18455407 125 Muscarinic antagonists with multiple stereocenters: Synthesis, affinity profile and functional activity of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine sulfoxide derivatives.EBI Universit£ di Firenze
17149881 3 Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the binding and activity at muscarinic receptor subtEBI The University of Toledo
12657274 109 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott Laboratories
12182854 45 A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.EBI Universit£ Libre de Bruxelles
23099092 74 Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.EBI GlaxoSmithKline
22959245 175 As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs).EBI The University of Sydney
22329602 22 Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.EBI University of Strasburg
23062550 59 Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists.EBI Vanderbilt University Medical Center
22335555 43 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.EBI NeurAxon Inc
24900202 38 Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI TBA
22148748 23 Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.EBI Vanderbilt University Medical Center
22677319 64 Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.EBI H. Lundbeck A/S
22749871 92 Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.EBI Vanderbilt University Medical Center
22243489 75 1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists.EBI Universit£ di Camerino
22475308 3 Bis-spirolabdane diterpenoids from Leonotis nepetaefolia.EBI University of Mississippi
22607684 50 7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.EBI The University of Sydney
22542010 31 Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI Amgen Inc
22313227 78 Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.EBI National Institute of Mental Health
22507963 73 Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.EBI Vanderbilt University Medical Center
22460029 21 Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
19630384 32 Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
21207959 69 Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.EBI National Institute of Mental Health
20875743 90 Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity relaEBI Pfizer Inc
20931963 112 Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.EBI ASKA Pharmaceutical Co., Ltd
20684563 176 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.EBI H. Lundbeck A/S
19963380 38 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.EBI Hunter College and the Graduate Center of the City University of New York
19653626 111 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicycloEBI Rhône-Poulenc Rorer
18686943 28 Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.EBI Matrix Laboratories Limited
18468904 48 High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand.EBI Purdue University
18042383 20 Design and synthesis of a fluorescent muscarinic antagonist.EBI Pfizer Inc
17483457 58 A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI Abbott Laboratories
17889543 90 Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.EBI Universit£ degli Studi di Milano
16821774 86 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.EBI Ono Pharmaceutical Co., Ltd
16275087 78 Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.EBI UCB Pharma SA
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes for BioMedical Research
14998318 112 Selective optimization of side activities: another way for drug discovery.EBI Prestwick Chemical Inc.
11831911 15 Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.EBI Banyu Tsukuba Research Institute
9986705 290 Identification and characterization of m1 selective muscarinic receptor antagonists1.EBI Warner-Lambert Company
9622546 109 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.EBI National Institute of Diabetes and Digestive and Kidney Diseases
1956033 121 Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.EBI Research Triangle Institute
2153827 12 Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides.EBI NIDDK
15203136 39 (+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI Virginia Commonwealth University
10450949 24 Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.EBI Wyeth-Ayerst Research
9873472 102 Identification and characterization of m4 selective muscarinic antagonists.EBI Parke-Davis Pharmaceutical Research
22197142 42 Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.EBI Vanderbilt University Medical Center
21930376 92 Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.EBI Vanderbilt University Medical Center
21870878 61 Inhalation by design: novel tertiary amine muscarinic M3 receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.EBI Pfizer Inc
21863888 9 Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.EBI Pfizer Inc
21524581 105 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.EBI Rhône-Poulenc Rorer
21194936 39 Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.EBI Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core
21075627 26 Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.EBI Pfizer Inc
21195614 56 Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.EBI Pfizer Inc
21310610 63 Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.EBI Theravance, Inc.
20716489 12 FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.EBI University of Wuerzburg
21146989 46 Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI The University of Sydney
20812727 157 Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.EBI National Institute of Mental Health
20801651 25 Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.EBI Vanderbilt University Medical Center
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20591666 66 A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI Università degli Studi di Milano
20384344 42 Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI Meiji Seika Kaisha, Ltd
20202841 47 Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.EBI Vanderbilt University Medical Center
20137933 218 Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.EBI Amgen Inc
20043678 92 Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.EBI Pfizer Inc
20004578 28 Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.EBI Vanderbilt University Medical Center
19646882 72 Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.EBI University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and the Informatics Institute of UMDNJ
19646865 45 Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.EBI Pfizer Inc
19663387 29 Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences Inc
19616944 27 Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.EBI GlaxoSmithKline
18922694 84 Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.EBI Johnson & Johnson PRD
 14 Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligandsEBI TBA
 32 The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI TBA
 37 The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.EBI TBA
 31 3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonistsEBI TBA
 74 New indole derivatives as potent and selective serotonin uptake inhibitorsEBI TBA
 88 A rationale for the design and synthesis of m1 selective muscarinic agonists.EBI TBA
19438238 45 Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.EBI Vanderbilt University Medical Center
19317446 51 Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
19208472 52 Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.EBI Novartis Institutes for BioMedical Research
18829311 74 Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.EBI Vanderbilt University Medical Center
18805692 99 Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.EBI Vanderbilt University Medical Center
18701276 97 Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI Merck Research Laboratories
18621528 133 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.EBI Pfizer Inc
18507369 85 Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.EBI Theravance, Inc.
16038549 20 Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.EBI Mitsubishi Pharma Corporation
15844951 5 Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.EBI Mitsubishi Pharma Corporation
18032038 38 Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.EBI UCB Pharma SA
17911022 108 Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
17571866 49 Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.EBI National Institute of Mental Health
17398090 18 Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.EBI UCB Pharma SA
17352463 59 Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).EBI Via Zambeletti 25
17352462 90 Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).EBI Via Zambeletti 25
17188867 66 1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.EBI Mitsubishi Pharma Corporation
16970392 91 Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.EBI Tsukuba Research Institute
16789729 25 A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.EBI Neurocrine Biosciences Inc
16722631 87 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.EBI Predix Pharmaceuticals Ltd.
16458504 37 Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI Columbia University College of Physicians and Surgeons
16439121 46 First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.EBI UCB Pharma SA
16392798 46 Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI Columbia University College of Physicians and Surgeons
16143528 213 Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI Columbia University College of Physicians and Surgeons
15115380 24 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoniEBI Schering-Plough Research Institute
14643338 124 Binding of beta-carbolines at 5-HT(2) serotonin receptors.EBI Virginia Commonwealth University
12798328 87 Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
12747793 32 C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.EBI University of North Carolina at Chapel Hill
11708906 15 Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.EBI University of Bologna
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
11150173 120 A potent, long-acting, orally active (2R)-2-[(1R)-3, 3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: novel muscarinic M(3) receptor antagonist with high selectivity for M(3) over M(2) receptors.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
11055330 30 Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.EBI Schering-Plough Research Institute
11012031 57 Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.EBI Schering-Plough Research Institute
10891110 87 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.EBI National Institute of Diabetes and Digestive and Kidney Diseases
10450976 1 Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.EBI Banyu Tsukuba Research Institute in collaboration with Merck Research Laboratories
9438027 30 Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.EBI Novo Nordisk A/S
9435896 36 Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.EBI SmithKline Beecham Pharmaceuticals Ltd
26565745 165 Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI Janssen Pharmaceutica N.V.
24088171 19 Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
23523385 73 Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.EBI Walter Reed Army Institute of Research
7783150 33 Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.EBI Royal Danish School of Pharmacy
21075638 105 Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.EBI Drug Discovery Laboratory AS
17084634 24 Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.EBI Universit£ degli Studi di Camerino
16539379 95 Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.EBI Universit£ di Firenze
16153841 24 Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists.EBI Shanghai Second Medical University
12593665 188 Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.EBI Johannes Gutenberg-University of Mainz
12086495 130 Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.EBI Pfizer Inc.
9371246 159 Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.EBI Uppsala University
8765510 100 3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.EBI Uppsala University
8057272 33 Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.EBI Glaxo Research and Development Ltd.
3712371 49 A novel class of conformationally restricted heterocyclic muscarinic agonists.EBI TBA
29324345 122 Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.EBI Shanghai Institute of Materia Medica
30258541 94 VU6007477, a Novel MEBI Vanderbilt Univercity
29089231 49 Challenges in the development of an MEBI Vanderbilt University School of Medicine
30052039 172 Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties.EBI Emory University
29656199 148 Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI University of Texas at Austin
29795757 100 Discovery of EBI Emory University
29456793 72 Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.EBI Emory University
29348805 56 Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists.EBI Emory University
29631962 252 Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.EBI Phenex Pharmaceuticals AG
28609709 75 Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.EBI Universit£ di Camerino
28633897 73 Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.EBI Vanderbilt University School of Medicine
28388054 72 Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the MEBI University of Regensburg
29589445 154 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DEBI Universit£ di Camerino
1674541 24 Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.EBI Harvard Medical School
1560441 35 Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).EBI Institute of Research
28442253 68 Optimization of MEBI Vanderbilt University Medical Center
29094937 194 Structure-Based Design and Discovery of New MEBI University of California
28598634 26 Design and Synthesis of?- and?-Lactam MEBI Pfizer Inc
28427812 74 Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.EBI Vanderbilt University School of Medicine
22050606 36 a-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters.BDB Dumlupinar University
28160944 6 Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.BDB Jaipur National University
26833890 18 Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.BDB Yogi Vemana University
23548908 1 Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.BDB University of Washington
26077890 33 Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.BDB Tehran University of Medical Sciences
26174207 21 Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.BDB The Johns Hopkins University School of Medicine
10421757 5 Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.BDB Institute of Genetics and Molecular and Cellular Biology (IGBMC)
19457661 21 Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.BDB Banyu Pharmaceutical Co.
18247549 45 Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes.BDB Schering-Plough Research Institute
17451234 12 Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.BDB Astex
12773052 14 Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.BDB Sapienza University of Rome
8494379 4 In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.BDB National Cancer Institute-Bethesda
15725032 3 Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.BDB University of North Carolina