BindingDB logo
myBDB logout

285 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
1732545 27 Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.EBI University of Uppsala
1507199 8 Synthesis and pharmacological evaluation of enantiomerically pure 4-deoxy-4-fluoromuscarines.EBI C.N.R.-Centro Studio Sostanze Organiche Naturali
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
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
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
25893046 77 Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.EBI Bristol-Myers Squibb Co.
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
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
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
25241924 47 The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.EBI Novartis Institutes for BioMedical Research
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
23953189 53 Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.EBI Pfizer Inc
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
13678406 7 Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.EBI The University of Toledo
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
17305327 5 Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.EBI Universit£ di Firenze
9548813 53 The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.EBI SmithKline Beecham Pharmaceuticals Ltd
7932564 38 Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines.EBI University of Bologna
2909747 50 Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.EBI University of Camerino
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
23116186 68 Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).EBI AstraZeneca
22931505 69 Chemokine receptor antagonists.EBI National Heart and Lung Institute
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
21062081 47 Histamine H3 receptor as a drug discovery target.EBI TBA
24900202 38 Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI TBA
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
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
22230199 12 Unbiased binding assays for discovering small-molecule probes and drugs.EBI Broad Institute of Harvard and MIT
21634396 55 Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.EBI Cephalon Inc
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
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
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
11585444 295 From hit to lead. Analyzing structure-profile relationships.EBI Universities of Lille
9986705 290 Identification and characterization of m1 selective muscarinic receptor antagonists1.EBI Warner-Lambert Company
10354408 58 1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.EBI Novo Nordisk A/S
9622546 109 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.EBI National Institute of Diabetes and Digestive and Kidney Diseases
7562938 17 New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.EBI Wyeth-Ayerst Research
8057277 54 Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.EBI National Institute on Drug Abuse-Intramural Research Program
2016720 4 Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.EBI Research Triangle Institute
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
9873644 74 Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.EBI Novo Nordisk A/S
9873472 102 Identification and characterization of m4 selective muscarinic antagonists.EBI Parke-Davis Pharmaceutical Research
 8 The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptorEBI TBA
22226656 75 Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.EBI Cephalon Inc
22197136 29 Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.EBI Cephalon Inc
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
21788137 33 N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI The University of Sydney
21865048 29 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.EBI Dainippon Sumitomo Pharma Co., Ltd
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
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
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
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
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
19199480 6 Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.EBI Sirtris Pharmaceuticals
18922694 84 Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.EBI Johnson & Johnson PRD
7673927 6 Isolation and Structure of Two Novel Muscarinic Receptor AntagonistsEBI TBA
8496700 16 The Role of Receptor Binding in Drug DiscoveryEBI TBA
 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
 8 Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.EBI TBA
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
18817368 57 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI Merck Research Laboratories
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
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
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
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
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
16134937 154 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.EBI 7TM Pharma A/S
15225708 32 Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.EBI Schering-Plough Research Institute
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
15026073 28 Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.EBI 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
12565973 33 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.EBI Schering-Plough Research Institute
12459007 13 Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.EBI Schering-Plough Research Institute
12086500 59 Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.EBI Schering-Plough Research Institute
11909724 35 Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.EBI Schering-Plough Research Institute
11859005 24 Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.EBI Schering-Plough Research Institute
11859004 18 Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.EBI Schering-Plough Research Institute
11708906 15 Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.EBI University of Bologna
11585438 21 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.EBI Schering-Plough Research Institute
11527721 12 Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.EBI Schering-Plough Research Institute
11514156 28 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.EBI Schering-Plough Research Institute
11378358 254 Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI Columbia University College of Physicians and Surgeons
11294385 21 Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.EBI Schering-Plough Research Institute
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
11133078 20 Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.EBI Schering-Plough Research Institute
11055332 42 Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.EBI Schering-Plough Research Institute
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
27503678 32 Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.EBI Vanderbilt University
27438064 29 Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
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
10612600 14 First fatty acylated dipeptides to affect muscarinic receptor ligand binding.EBI University of Toledo
30682248 15 Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).EBI School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
32342685 325 Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective DEBI National Institute of Neurological Disorders and Stroke
10498210 27 A new class of selective and potent inhibitors of neuronal nitric oxide synthase.EBI Pfizer Inc
31074983 202 Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines MEBI University of Regensburg
31021617 136 Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI University of Pennsylvania
30875219 254 Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine DEBI University of North Carolina at Chapel Hill
31204225 55 Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.EBI National Institute of Advanced Industrial Science and Technology (AIST)
31248774 45 SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic MEBI Vanderbilt University
10206558 50 Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.EBI Schering-Plough Research Institute
30554957 105 Muscarinic agonist, ()-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human MEBI University of Kentucky
31185168 144 Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI RTI International
9651157 52 Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.EBI Warner-Lambert Company
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
31613617 195 Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine DEBI Friedrich-Alexander-Universit£t Erlangen-N£rnberg
31620230 283 3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HTEBI University of Minnesota Twin Cities
31223452 49 Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.EBI Pfizer Inc.
26565745 165 Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI Janssen Pharmaceutica N.V.
25051097 77 Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.EBI University of W£rzburg
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
7990109 62 Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.EBI H. Lundbeck A/S
7853341 115 3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.EBI Uppsala University
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
32353859 59 A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.EBI QBI COVID-19 Research Group (QCRG)
18182302 69 Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.EBI Universit£ di Milano
17289384 38 Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists.EBI Shanghai Jiao Tong University School of Medicine
17084634 24 Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.EBI Universit£ degli Studi di Camerino
16387499 15 6H,13H-Pyrazino[1,2-a;4,5-a']diindole analogs: probing the pharmacophore for allosteric ligands of muscarinic M2 receptors.EBI University of W£rzburg
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
12166953 9 Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators.EBI University of Bonn
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
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
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
28522253 83 Challenges in the development of an MEBI Vanderbilt University School of Medicine
1578479 24 Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.EBI Uppsala University
1560441 35 Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).EBI Institute of Research
1548680 12 Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.EBI Merck Sharp and Dohme Research Laboratories
28442253 68 Optimization of MEBI Vanderbilt University Medical Center
28408223 5 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.EBI IntelliSyn Pharma
1507203 96 Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.EBI University of South Carolina
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
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
26518975 9 Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB Peking University
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
26469307 7 Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB University of Leipzig
26390252 12 Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.BDB Dana-Farber Cancer Institute Inc
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
25462626 6 Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes.BDB COMSATS Institute of Information Technology
23547776 25 Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.BDB Massachusetts Institute of Technology
16480269 9 Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors.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