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109 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
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
Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.EBI
Astellas Pharma
The effect of absolute configuration on activity, subtype selectivity (M3/M2) of 3a-acyloxy-6ß-acetoxyltropane derivatives as muscarinic M3 receptor antagonists.EBI
Shanghai Jiao Tong University
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
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
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.EBI
University Of Bologna
Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.EBI
Kyorin Pharmaceutical
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.EBI
Kyorin Pharmaceutical
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.EBI
Vanderbilt Institute Of Chemical Biology
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.EBI
Ranbaxy Research Laboratories
Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.EBI
Astellas Pharma
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
5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists.EBI
Universit£
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.EBI
National Institute Of Diabetes And Digestive And Kidney Diseases
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties.EBI
University Of Catania
Stereoselective synthesis and biodistribution of potent [11C]-labeled antagonists for positron emission tomography imaging of muscarinic receptors in the airways.EBI
Groningen University Hospital
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.EBI
National Institutes Of Health
Resolution and in vitro and initial in vivo evaluation of isomers of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate: a high-affinity ligand for the muscarinic receptor.EBI
Oak Ridge National Laboratory (Ornl)
Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.EBI
Albany Molecular Research
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.EBI
Oak Ridge National Laboratory
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.EBI
Medical Research Division Of American Cyanamid
Synthesis and structure-activity studies of a series of spirooxazolidine-2,4-diones: 4-oxa analogues of the muscarinic agonist 2-ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione.EBI
Institute For Drug Discovery Research
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.EBI
Research Triangle Institute
Muscarinic receptor binding profile of para-substituted caramiphen analogues.EBI
Virginia Commonwealth University
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric replacement of classical cationic heads.EBI
Istituto De Angeli
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.EBI
Institute Of Research
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.EBI
Nova Pharmaceutical
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.EBI
Royal Danish School Of Pharmacy
 
Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivativesEBI
TBA
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.EBI
Vanderbilt University Medical Center
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
 
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorineEBI
TBA
 
Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analogEBI
TBA
 
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivityEBI
TBA
 
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptorsEBI
TBA
 
Muscarinic receptor probes based on amine congeners of pirenzepine and telenzepineEBI
TBA
 
Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5EBI
TBA
 
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.EBI
TBA
 
Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpineEBI
TBA
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
Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.EBI
Ranbaxy Research Laboratories
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.EBI
Schering-Plough Research Institute
Synthesis and binding studies of some epibatidine analogues.EBI
Institute Of Pharmacy And Biochemistry
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.EBI
Dipartimento Di Scienze Farmaceutiche - Università
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.EBI
University Of Camerino
Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.EBI
Yamanouchi Pharmaceutical
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.EBI
Hoechst-Roussel Pharmaceuticals
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.EBI
Solvay Duphar
Construction of a molecular shape analysis-three-dimensional quantitative structure-analysis relationship for an analog series of pyridobenzodiazepinone inhibitors of muscarinic 2 and 3 receptors.EBI
College Of Pharmacy
Preparation of 18F-labeled muscarinic agonist with M2 selectivity.EBI
National Institutes Of Health
Syntheses and biological properties of chiral fluoroalkyl quinuclidinyl benzilates.EBI
National Institutes Of Health
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.EBI
Dr. Karl Thomae
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.EBI
Dr. Karl Thomae
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.EBI
Niddk
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.EBI
Sandoz Pharma
Synthesis and pharmacological investigation of the enantiomers of muscarone and allomuscarone.EBI
Istituto Chimico-Farmaceutico Dell'Università
Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.EBI
Abbott Laboratories
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.EBI
University Of South Carolina
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.BDB
University Of Washington
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.BDB
Dana-Farber Cancer Institute
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).BDB
Oregon Health & Science University
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.BDB
University Of Wisconsin-Madison
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.BDB
University Of North Carolina At Chapel Hill
Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.BDB
University Of North Carolina At Chapel Hill
New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.BDB
Silesian University Of Technology