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, 1,346K data for 622K 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

247 articles for thisTarget


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

PMID
Data
Article Title
Organization
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.EBI
Ghent University
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.EBI
University Of Mainz
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
Challenges in the development of an MEBI
Vanderbilt University Medical Center
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.EBI
University Of Kansas
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
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)
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.EBI
Vanderbilt University Medical Center
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
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.EBI
Aptuit
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI
Aptuit
Design and optimization of selective azaindole amide M1 positive allosteric modulators.EBI
Pfizer
Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists.EBI
Sumitomo Dainippon Pharma
Muscarinic acetylcholine receptor binding affinities of pethidine analogs.EBI
University Of Kentucky
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
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.EBI
City University Of New York
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.EBI
Novartis Institutes For Biomedical Research
Pyrrolopyridine or Pyrazolopyridine Derivatives.EBI
Temple University School Of Pharmacy
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
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.EBI
Boehringer Ingelheim Pharma
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.EBI
Bristol-Myers Squibb
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.EBI
University Of W£Rzburg
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI
Jagiellonian University Collegium Medicum
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.EBI
RhôNe-Poulenc Rorer
Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists.EBI
Korea Institute Of Science And Technology
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.EBI
Universit£
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
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI
Glaxosmithkline
Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists.EBI
Dainippon Sumitomo Pharma
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
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£
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 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)
Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists.EBI
Dainippon Sumitomo Pharma
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£
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
Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists.EBI
Dainippon Sumitomo Pharma
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
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.EBI
Vanderbilt University Medical Center
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 evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.EBI
University Of Minnesota
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
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
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.EBI
University Of Strasburg
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays.EBI
University Of Strasburg
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
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.EBI
TBA
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.EBI
Vanderbilt University Medical Center
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
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
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
Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
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
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.EBI
Boehringer Ingelheim Pharma
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£
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.EBI
National Institute On Drug Abuse-Intramural Research Program
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.EBI
Novartis Institutes For Biomedical Research
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.EBI
Umr Cnrs/Ulp 7081
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
Current and novel approaches to the drug treatment of schizophrenia.EBI
Merck Sharp And Dohme Research Laboratories
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
(+/-)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
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.EBI
Argenta Discovery
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.EBI
Florida A&M University
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.EBI
Vanderbilt University Medical Center
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
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
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
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
Progress in structure based drug design for G protein-coupled receptors.EBI
Heptares Therapeutics
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.EBI
TBA
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.EBI
RhôNe-Poulenc Rorer
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
FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.EBI
University Of Wuerzburg
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
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
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.EBI
Neurocrine Biosciences
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
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
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
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
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 novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI
Tsukuba Research Institute
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI
Neurocrine Biosciences
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
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
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
 
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)EBI
TBA
 
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
 
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivityEBI
TBA
 
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonistsEBI
TBA
 
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptorsEBI
TBA
 
New indole derivatives as potent and selective serotonin uptake inhibitorsEBI
TBA
 
SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndromeEBI
TBA
 
A rationale for the design and synthesis of m1 selective muscarinic agonists.EBI
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
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
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
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI
Amgen
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
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
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
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.EBI
Ucb Pharma
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI
Pfizer
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
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.EBI
Cerep
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
A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.EBI
Neurocrine Biosciences
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI
Pfizer
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
On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.EBI
Umr Cnrs/Ulp 7081
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
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.EBI
Astrazeneca
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
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
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
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.EBI
Schering-Plough Research Institute
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
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.EBI
University Of Bologna
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.EBI
Seoul National University
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.EBI
Columbia University College Of Physicians And Surgeons
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
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
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.EBI
Institute Of Science And Technology
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.EBI
University Of GöTeborg
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
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.EBI
Eli Lilly
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
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.EBI
University Of Groningen
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
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
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
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
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
Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.BDB
The Johns Hopkins University School Of Medicine
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.BDB
University Of Newcastle
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.BDB
Sapienza University Of Rome