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282 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
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
27502700 36 Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.EBI Novartis Institutes of Biomedical Research (NIBR)
27173801 29 Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.EBI Vanderbilt University Medical Center
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
26631313 20 Design and optimization of selective azaindole amide M1 positive allosteric modulators.EBI Pfizer Inc
26428869 7 Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists.EBI Sumitomo Dainippon Pharma Co., Ltd
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
26227772 22 C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.EBI City University of New York
26191365 49 Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.EBI Novartis Institutes for BioMedical Research
26191354 20 Pyrrolopyridine or Pyrazolopyridine Derivatives.EBI Temple University School of Pharmacy
26112443 84 Design, synthesis and evaluation of MCH receptor 1 antagonists--Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
26077492 92 Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
25893046 77 Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.EBI Bristol-Myers Squibb Co.
25478907 29 Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.EBI University of W£rzburg
25557493 109 Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI Jagiellonian University Collegium Medicum
25800115 62 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.EBI Rhône-Poulenc Rorer
25765911 9 Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists.EBI Korea Institute of Science and Technology
24980056 44 Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.EBI Universit£ di Camerino
24916029 42 Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2.EBI Astellas Pharma Inc
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
24856064 9 Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
25435150 40 Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.EBI Vanderbilt University Medical Center
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
24856614 6 Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M1 muscarinic acetylcholine receptor.EBI Monash University (Parkville Campus)
24852118 7 Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
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
23416001 32 Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.EBI Vanderbilt University Medical Center
24900656 9 Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
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
23237839 23 Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.EBI Vanderbilt University Medical Center
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
17977730 42 Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.EBI University of Minnesota
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
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
12657274 109 Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.EBI Abbott Laboratories
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[5.4.1.0(2,6).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
22984902 59 Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.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
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
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
20188547 152 Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences Inc
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
18485703 37 3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
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
16213721 60 N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.EBI National Institute on Drug Abuse-Intramural Research Program
16198561 99 Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI Novartis Institutes for BioMedical Research
15294002 18 Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.EBI UMR CNRS/ULP 7081
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
11170639 73 Current and novel approaches to the drug treatment of schizophrenia.EBI Merck Sharp and Dohme Research Laboratories
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[2.2.1.0(2,6)]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
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
22177783 122 Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.EBI Argenta Discovery Ltd
22245230 128 Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI Florida A&M University
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
22153347 111 Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia.EBI Neurocrine Biosciences Inc
22030026 13 Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.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
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
21615150 14 Progress in structure based drug design for G protein-coupled receptors.EBI Heptares Therapeutics Limited
24900216 33 Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.EBI TBA
21524581 105 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.EBI Rhône-Poulenc Rorer
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
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
20347297 61 The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.EBI Neurocrine Biosciences Inc
20227880 144 Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences Inc
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
20156687 7 Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.EBI Vanderbilt University Medical Center
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
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
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
19553115 96 Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences 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
19588934 71 Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.EBI Abbott Laboratories
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
 14 Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivityEBI TBA
 31 3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonistsEBI TBA
 24 Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptorsEBI TBA
 45 SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndromeEBI TBA
 88 A rationale for the design and synthesis of m1 selective muscarinic agonists.EBI TBA
 40 Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5EBI 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
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
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc
18595716 142 Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.EBI Florida A&M University
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
18052023 30 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
18032038 38 Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.EBI UCB Pharma SA
17976986 80 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI Pfizer Inc
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
17448659 29 Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.EBI Cerep
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
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Inc
16302823 7 On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.EBI UMR CNRS/ULP 7081
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
15582404 68 Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.EBI AstraZeneca
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
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
12617901 23 2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.EBI F. Hoffmann-La Roche Inc
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
11741475 56 Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.EBI The University of Toledo
11708906 15 Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.EBI University of Bologna
11597415 36 Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.EBI Seoul National University
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
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
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
10522693 14 Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.EBI Institute of Science and Technology
10377229 107 New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI University of Göteborg
10206558 50 Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.EBI Schering-Plough Research Institute
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
9464368 78 1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.EBI Eli Lilly and 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
9406603 49 Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI University of Groningen
26565745 165 Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI Janssen Pharmaceutica N.V.
24900754 2 Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1.EBI Montclair State University
23718562 3 Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.EBI Monash University
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
18182302 69 Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.EBI Universit£ di Milano
17880057 131 Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.EBI Solvay Pharma
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
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
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.
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.
30383372 190 Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI Huazhong University of Science and Technology
30431269 41 Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.EBI Pfizer Inc.
30258541 94 VU6007477, a Novel MEBI Vanderbilt Univercity
29716781 28 Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program.EBI Pfizer Inc.
29544056 3 Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the MEBI Monash University (Parkville Campus)
29533874 76 The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.EBI University of Defence
29146472 71 Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor.EBI Roche Pharma Research and Early Development
29089231 49 Challenges in the development of an MEBI Vanderbilt University School of Medicine
29656199 148 Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.EBI University of Texas at Austin
29754948 69 The discovery of VU0486846: steep SAR from a series of MEBI Vanderbilt University Medical Center
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
28958623 35 Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HEBI GlaxoSmithKline
28763213 193 Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.EBI Jagiellonian University Medical College
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
28442253 68 Optimization of MEBI Vanderbilt University Medical Center
1433209 58 Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.EBI Eli Lilly and Company
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
28389149 56 Discovery of selective, orally bioavailable, N-linked arylsulfonamide NaEBI Department of Discovery Chemistry Merck & Co.
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
26851737 36 One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.BDB University of Karachi
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
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
9223589 17 N-(3-lodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(3',4'-dichloro phenyl)nortropane (beta-CDIT), a tropane derivative: pharmacological characterization as a specific ligand for the dopamine transporter in the rodent brain.BDB University of Tours
7616416 11 7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity.BDB Third Tokushima Institute of New Drug Research
15006388 34 Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.BDB Hoffmann-La Roche Inc
10956187 18 Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.BDB University of Newcastle
12773052 14 Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.BDB Sapienza University of Rome