The first public molecular recognition database, BindingDB supports research, education and practice in drug discovery, pharmacology and related fields.

BindingDB contains 2.8M data for 1.2M Compounds and 9.2K Targets. Of those, 1,339K data for 617K Compounds and 4.5K Targets were curated by BindingDB curators. BindingDB is a FAIRsharing resource.

If BindingDB was of value to your research, please take a moment to donate to this nonprofit project. Your donation will let us provide you with more data and improved service.

Advanced Search

211 articles for thisTarget


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

PMID
Data
Article Title
Organization
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
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
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.EBI
Pfizer
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.EBI
Eli Lilly
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.EBI
Bristol-Myers Squibb
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.EBI
RhôNe-Poulenc Rorer
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.EBI
Universit£
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
Glaxosmithkline
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£
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
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
Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.EBI
Keio University
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI
Adamed
Antagonists of the kappa opioid receptor.EBI
The Scripps Research Institute
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£
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.EBI
Pfizer
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
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
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
The discovery of AZD9164, a novel muscarinic M3 antagonist.EBI
Astrazeneca
The discovery of new spirocyclic muscarinic M3 antagonists.EBI
Astrazeneca
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
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.EBI
Glaxosmithkline
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.EBI
Glaxosmithkline
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.EBI
Universit£
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.EBI
Universita Di Firenze
M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.EBI
Glaxosmithkline
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.EBI
Glaxosmithkline
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.EBI
Universit£
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
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
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£
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
A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.EBI
Universit£
 
Design, synthesis and biological activity of some 4-DAMP- related compoundsEBI
TBA
Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.EBI
Glaxosmithkline
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
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).EBI
Astrazeneca
Chemokine receptor antagonists.EBI
National Heart And Lung Institute
Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists.EBI
Vanderbilt University Medical Center
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
Histamine H3 receptor as a drug discovery target.EBI
TBA
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI
TBA
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
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.EBI
Vanderbilt University Medical Center
1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists.EBI
Universit£
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.EBI
The University Of Sydney
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.EBI
Amgen
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
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.EBI
Vanderbilt University Medical Center
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Unbiased binding assays for discovering small-molecule probes and drugs.EBI
Broad Institute Of Harvard And Mit
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
Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
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
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
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
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
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
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
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
Design and synthesis of a fluorescent muscarinic antagonist.EBI
Pfizer
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.EBI
Abbott Laboratories
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.EBI
Universit£
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.EBI
Ucb Pharma
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes For Biomedical Research
Selective optimization of side activities: another way for drug discovery.EBI
Prestwick Chemical
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.EBI
Banyu Tsukuba Research Institute
From hit to lead. Analyzing structure-profile relationships.EBI
Universities Of Lille
Identification and characterization of m1 selective muscarinic receptor antagonists1.EBI
Warner-Lambert
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
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.EBI
National Institute Of Diabetes And Digestive And Kidney Diseases
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.EBI
Wyeth-Ayerst Research
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.EBI
National Institute On Drug Abuse-Intramural Research Program
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.EBI
Research Triangle Institute
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.EBI
Institute Of Research
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.EBI
Virginia Commonwealth University
Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.EBI
Wyeth-Ayerst Research
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.EBI
Novo Nordisk
Identification and characterization of m4 selective muscarinic antagonists.EBI
Parke-Davis Pharmaceutical Research
 
The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptorEBI
TBA
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
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.EBI
Cephalon
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.EBI
Vanderbilt University Medical Center
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.EBI
Vanderbilt University Medical Center
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
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.EBI
The University Of Sydney
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
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.EBI
RhôNe-Poulenc Rorer
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
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.EBI
The University Of Sydney
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
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.EBI
Vanderbilt University Medical Center
Spiroindolones, a potent compound class for the treatment of malaria.EBI
Swiss Tropical And Public Health Institute
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.EBI
Università
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
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
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
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.EBI
Sirtris Pharmaceuticals
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.EBI
Johnson & Johnson Prd
Isolation and Structure of Two Novel Muscarinic Receptor AntagonistsEBI
TBA
The Role of Receptor Binding in Drug DiscoveryEBI
TBA
 
Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligandsEBI
TBA
 
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonistsEBI
TBA
 
A rationale for the design and synthesis of m1 selective muscarinic agonists.EBI
TBA
 
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.EBI
TBA
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.EBI
Novartis Institutes For Biomedical Research
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
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI
Merck Research Laboratories
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
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
Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.EBI
Mitsubishi Pharma
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.EBI
Mitsubishi Pharma
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.EBI
Ucb Pharma
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.EBI
Glaxosmithkline
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
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).EBI
Via Zambeletti 25
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).EBI
Via Zambeletti 25
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.EBI
Mitsubishi Pharma
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.EBI
Tsukuba Research Institute
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
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
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
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.EBI
Columbia University College Of Physicians And Surgeons
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.EBI
7Tm Pharma
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.EBI
Schering-Plough Research Institute
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
Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.EBI
Schering-Plough Research Institute
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
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
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.EBI
Schering-Plough Research Institute
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
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
Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
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
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.EBI
Schering-Plough Research Institute
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.EBI
University Of Bologna
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
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.EBI
Schering-Plough Research Institute
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.EBI
Schering-Plough Research Institute
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI
Columbia University College Of Physicians And Surgeons
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
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
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.EBI
Schering-Plough Research Institute
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.EBI
Schering-Plough Research Institute
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
First fatty acylated dipeptides to affect muscarinic receptor ligand binding.EBI
University Of Toledo
A new class of selective and potent inhibitors of neuronal nitric oxide synthase.EBI
Pfizer
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.EBI
Schering-Plough Research Institute
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
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
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
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
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.EBI
Uppsala University
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.EBI
Royal Danish School Of Pharmacy
Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.EBI
Uppsala University
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).EBI
Institute Of Research
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
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.EBI
University Of South Carolina
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
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.BDB
University Of Washington
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.BDB
Peking University
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
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.BDB
University Of Leipzig
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.BDB
Dana-Farber Cancer Institute
Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.BDB
The Johns Hopkins University School Of Medicine
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
Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.BDB
Massachusetts Institute Of Technology