302 articles for thisTarget

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

PMID	Data	Article Title	Organization
1732545	27	Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.	University of Uppsala
1507199	8	Synthesis and pharmacological evaluation of enantiomerically pure 4-deoxy-4-fluoromuscarines.	C.N.R.-Centro Studio Sostanze Organiche Naturali
1995893	81	Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships.	Ferrosan
2299626	18	Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.	University of Uppsala
2258904	21	Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.	Uppsala University
3346873	24	Derivatives of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.	University of Uppsala
3336015	8	Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.	University of California
3494849	3	6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.	TBA
12113806	40	Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.	Ghent University
11354386	90	Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.	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-CH	Jagiellonian University Medical College
27939174	84	Challenges in the development of an M	Vanderbilt University Medical Center
27839919	192	Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.	University of Kansas
27185330	60	Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.	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.	Jagiellonian University Medical College
26471092	23	Molecular hybridization yields triazole bronchodilators for the treatment of COPD.	Pfizer
26299349	66	Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.	Eli Lilly
25893046	77	Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.	Bristol-Myers Squibb
25800115	62	Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.	RhôNe-Poulenc Rorer
24980056	44	Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.	Universit£
24881566	140	Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).	Glaxosmithkline
25275964	171	Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).	Universit£
25241924	47	The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.	Novartis Institutes For Biomedical Research
25147929	105	Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).	Vanderbilt University Medical Center
24844758	6	Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.	Keio University
24805037	380	Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.	Adamed
24690494	92	Antagonists of the kappa opioid receptor.	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.	Universit£
23953189	53	Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.	Pfizer
23379472	187	Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.	University of Arkansas For Medical Sciences
23200253	67	Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism.	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.	Vanderbilt University Medical Center
13678406	7	Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.	The University of Toledo
22047691	76	The discovery of AZD9164, a novel muscarinic M3 antagonist.	Astrazeneca
21036043	78	The discovery of new spirocyclic muscarinic M3 antagonists.	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.	Glaxosmithkline
20483611	89	2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.	Glaxosmithkline
20483599	81	2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.	Glaxosmithkline
19896386	85	Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.	Universit£
19928767	88	Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.	Universita Di Firenze
19243945	73	M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.	Glaxosmithkline
18818072	162	Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.	Glaxosmithkline
18798607	27	Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.	Glaxosmithkline
18543900	105	Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.	Universit£
18680280	34	Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.	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.	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.	Universit£
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.	Smithkline Beecham Pharmaceuticals
12657274	109	Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.	Abbott Laboratories
12182854	45	A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold.	Universit£
23099092	74	Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.	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).	The University of Sydney
23116186	68	Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).	Astrazeneca
22931505	69	Chemokine receptor antagonists.	National Heart and Lung Institute
23062550	59	Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists.	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.	Neuraxon
21062081	47	Histamine H3 receptor as a drug discovery target.	TBA
24900202	38	Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.	TBA
22677319	64	Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.	H. Lundbeck
22749871	92	Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.	Vanderbilt University Medical Center
22243489	75	1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists.	Universit£
22607684	50	7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.	The University of Sydney
22542010	31	Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition.	Amgen
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.	National Institute of Mental Health
22507963	73	Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.	Vanderbilt University Medical Center
22460029	21	Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.	Glaxosmithkline
22230199	12	Unbiased binding assays for discovering small-molecule probes and drugs.	Broad Institute of Harvard and Mit
21634396	55	Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.	Cephalon
19630384	32	Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.	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.	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 rela	Pfizer
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.	Aska Pharmaceutical
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.	H. Lundbeck
19963380	38	Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.	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-azoniabicyclo	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.	Purdue University
18042383	20	Design and synthesis of a fluorescent muscarinic antagonist.	Pfizer
17483457	58	A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.	Abbott Laboratories
17889543	90	Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.	Universit£
16275087	78	Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.	Ucb Pharma
16198561	99	Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.	Novartis Institutes For Biomedical Research
14998318	112	Selective optimization of side activities: another way for drug discovery.	Prestwick Chemical
11831911	15	Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.	Banyu Tsukuba Research Institute
11585444	295	From hit to lead. Analyzing structure-profile relationships.	Universities of Lille
9986705	290	Identification and characterization of m1 selective muscarinic receptor antagonists1.	Warner-Lambert
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.	Novo Nordisk
9622546	109	6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.	National Institute of Diabetes and Digestive and Kidney Diseases
7562938	17	New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.	Wyeth-Ayerst Research
8057277	54	Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.	National Institute On Drug Abuse-Intramural Research Program
2016720	4	Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.	Research Triangle Institute
1956033	121	Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.	Research Triangle Institute
2153827	12	Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides.	Niddk
15203136	39	(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.	Virginia Commonwealth University
10450949	24	Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.	Wyeth-Ayerst Research
9873644	74	Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.	Novo Nordisk
9873472	102	Identification and characterization of m4 selective muscarinic antagonists.	Parke-Davis Pharmaceutical Research
	8	The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptor	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.	Cephalon
22197136	29	Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.	Cephalon
22197142	42	Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.	Vanderbilt University Medical Center
21930376	92	Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.	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.	Pfizer
21788137	33	N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.	The University of Sydney
21865048	29	2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.	Dainippon Sumitomo Pharma
21524581	105	Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.	RhôNe-Poulenc Rorer
21194936	39	Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.	Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core
21146989	46	Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands.	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.	National Institute of Mental Health
20801651	25	Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.	Vanderbilt University Medical Center
20813948	63	Spiroindolones, a potent compound class for the treatment of malaria.	Swiss Tropical and Public Health Institute
20591666	66	A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.	Università
20202841	47	Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.	Vanderbilt University Medical Center
19646882	72	Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.	University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
19616944	27	Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.	Glaxosmithkline
19199480	6	Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.	Sirtris Pharmaceuticals
18922694	84	Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.	Johnson & Johnson Prd
7673927	6	Isolation and Structure of Two Novel Muscarinic Receptor Antagonists	TBA
8496700	16	The Role of Receptor Binding in Drug Discovery	TBA
	14	Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands	TBA
	32	The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)	TBA
	37	The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.	TBA
	31	3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists	TBA
	74	New indole derivatives as potent and selective serotonin uptake inhibitors	TBA
	88	A rationale for the design and synthesis of m1 selective muscarinic agonists.	TBA
	8	Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.	TBA
19317446	51	Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.	Glaxosmithkline
19208472	52	Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.	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.	Vanderbilt University Medical Center
18817368	57	Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.	Merck Research Laboratories
18805692	99	Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.	Vanderbilt University Medical Center
18507369	85	Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.	Theravance
16038549	20	Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.	Mitsubishi Pharma
15844951	5	Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.	Mitsubishi Pharma
18032038	38	Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives.	Ucb Pharma
17911022	108	Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists.	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.	National Institute of Mental Health
17352463	59	Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).	Via Zambeletti 25
17352462	90	Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).	Via Zambeletti 25
17188867	66	1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.	Mitsubishi Pharma
16970392	91	Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.	Tsukuba Research Institute
16722631	87	An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.	Predix Pharmaceuticals
16458504	37	Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.	Columbia University College of Physicians and Surgeons
16392798	46	Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.	Columbia University College of Physicians and Surgeons
16143528	213	Synthesis of potent and selective serotonin 5-HT1B receptor ligands.	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.	7Tm Pharma
15225708	32	Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.	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 antagoni	Schering-Plough Research Institute
15026073	28	Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.	Schering-Plough Research Institute
14643338	124	Binding of beta-carbolines at 5-HT(2) serotonin receptors.	Virginia Commonwealth University
12798328	87	Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2.	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.	University of North Carolina At Chapel Hill
12565973	33	Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.	Schering-Plough Research Institute
12459007	13	Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.	Schering-Plough Research Institute
12086500	59	Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.	Schering-Plough Research Institute
11909724	35	Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.	Schering-Plough Research Institute
11859005	24	Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.	Schering-Plough Research Institute
11859004	18	Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.	Schering-Plough Research Institute
11708906	15	Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.	University of Bologna
11585438	21	Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.	Schering-Plough Research Institute
11527721	12	Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.	Schering-Plough Research Institute
11514156	28	Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element.	Schering-Plough Research Institute
11378358	254	Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.	Columbia University College of Physicians and Surgeons
11294385	21	Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists.	Schering-Plough Research Institute
32374602	190	Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus.	Universit£
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.	Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
32227883	40	Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge	University of Mississippi
11133078	20	Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.	Schering-Plough Research Institute
32233403	135	Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M	University of Regensburg
32202101	120	Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.	Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
11055332	42	Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.	Schering-Plough Research Institute
11055330	30	Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.	Schering-Plough Research Institute
11012031	57	Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.	Schering-Plough Research Institute
27503678	32	Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.	Vanderbilt University
27438064	29	Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.	Boehringer Ingelheim Pharma
10891110	87	6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.	National Institute of Diabetes and Digestive and Kidney Diseases
10612600	14	First fatty acylated dipeptides to affect muscarinic receptor ligand binding.	University of Toledo
30682248	15	Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).	School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
32342685	325	Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D	National Institute of Neurological Disorders and Stroke
10498210	27	A new class of selective and potent inhibitors of neuronal nitric oxide synthase.	Pfizer
31074983	202	Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M	University of Regensburg
31021617	136	Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D	University of Pennsylvania
30875219	254	Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D	University of North Carolina At Chapel Hill
31204225	55	Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.	National Institute of Advanced Industrial Science and Technology (Aist)
31248774	45	SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M	Vanderbilt University
10206558	50	Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.	Schering-Plough Research Institute
30554957	105	Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M	University of Kentucky
31185168	144	Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.	Rti International
9651157	52	Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.	Warner-Lambert
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.	Novo Nordisk
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.	Smithkline Beecham Pharmaceuticals
31613617	195	Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D	Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
31620230	283	3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT	University of Minnesota Twin Cities
31223452	49	Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.	Pfizer
26565745	165	Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.	Janssen Pharmaceutica
25051097	77	Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.	University of W£Rzburg
24088171	19	Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.	Boehringer Ingelheim Pharma
7990109	62	Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.	H. Lundbeck
7853341	115	3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.	Uppsala University
23523385	73	Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.	Walter Reed Army Institute of Research
7783150	33	Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.	Royal Danish School of Pharmacy
21075638	105	Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.	Drug Discovery Laboratory
32353859	59	A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.	Qbi Covid-19 Research Group (Qcrg)
18182302	69	Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.	Universit£
17289384	38	Quantitative structure-selectivity relationship for M2 selectivity between M1 and M2 of piperidinyl piperidine derivatives as muscarinic antagonists.	Shanghai Jiao Tong University School of Medicine
17084634	24	Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.	Universit£
16387499	15	6H,13H-Pyrazino[1,2-a;4,5-a']diindole analogs: probing the pharmacophore for allosteric ligands of muscarinic M2 receptors.	University of W£Rzburg
16539379	95	Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.	Universit£
16153841	24	Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists.	Shanghai Second Medical University
12593665	188	Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.	Johannes Gutenberg-University of Mainz
12166953	9	Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators.	University of Bonn
12086495	130	Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.	Pfizer
9371246	159	Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.	Uppsala University
8765510	100	3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.	Uppsala University
8057272	33	Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.	Glaxo Research and Development
3712371	49	A novel class of conformationally restricted heterocyclic muscarinic agonists.	TBA
30258541	94	VU6007477, a Novel M	Vanderbilt Univercity
29089231	49	Challenges in the development of an M	Vanderbilt University School of Medicine
30052039	172	Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties.	Emory University
29656199	148	Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.	University of Texas At Austin
29795757	100	Discovery of	Emory University
29348805	56	Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists.	Emory University
29631962	252	Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.	Phenex Pharmaceuticals
28609709	75	Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.	Universit£
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.	Vanderbilt University School of Medicine
28388054	72	Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M	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 D	Universit£
1674541	24	Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.	Harvard Medical School
28522253	83	Challenges in the development of an M	Vanderbilt University School of Medicine
1578479	24	Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.	Uppsala University
1560441	35	Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).	Institute of Research
1548680	12	Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.	Merck Sharp and Dohme Research Laboratories
28442253	68	Optimization of M	Vanderbilt University Medical Center
28408223	5	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.	Intellisyn Pharma
1507203	96	Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.	University of South Carolina
29094937	194	Structure-Based Design and Discovery of New M	University of California
28598634	26	Design and Synthesis of?- and?-Lactam M	Pfizer
28427812	74	Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.	Vanderbilt University School of Medicine
26833890	18	Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.	Yogi Vemana University
23548908	1	Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis.	University of Washington
26518975	9	Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.	Peking University
26077890	33	Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.	Tehran University of Medical Sciences
26469307	7	Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.	University of Leipzig
26390252	12	Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.	Dana-Farber Cancer Institute
26174207	21	Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.	The Johns Hopkins University School of Medicine
25462626	6	Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes.	Comsats Institute of Information Technology
23547776	25	Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.	Massachusetts Institute of Technology
16480269	9	Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors.	Astex
12773052	14	Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.	Sapienza University of Rome