280 articles for thisTarget

---

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

PMID	Data	Article Title	Organization
27997171	48	Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.	The University of Newcastle
1732545	27	Phenyl-substituted analogues of oxotremorine as muscarinic antagonists.	University of Uppsala
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
27564135	499	1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.	Aptuit
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
26951894	376	1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.	Aptuit
26786693	153	Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.	Aptuit
26516782	59	Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.	University of Copenhagen
26494260	36	Muscarinic acetylcholine receptor binding affinities of pethidine analogs.	University of Kentucky
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
25629394	52	Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist..	Theravance Biopharma
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£
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£
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£
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
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£
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
22329602	22	Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.	University of Strasburg
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
24900202	38	Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.	TBA
22148748	23	Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.	Vanderbilt University Medical Center
22677319	64	Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.	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£
22475308	3	Bis-spirolabdane diterpenoids from Leonotis nepetaefolia.	University of Mississippi
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
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
18686943	28	Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.	Matrix Laboratories
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£
16821774	86	Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.	Ono Pharmaceutical
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
9986705	290	Identification and characterization of m1 selective muscarinic receptor antagonists1.	Warner-Lambert
9622546	109	6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.	National Institute of Diabetes and Digestive and Kidney Diseases
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
9873472	102	Identification and characterization of m4 selective muscarinic antagonists.	Parke-Davis Pharmaceutical Research
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
21863888	9	Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-ß2-agonist for the treatment of chronic obstructive pulmonary disease.	Pfizer
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
21075627	26	Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.	Pfizer
21195614	56	Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.	Pfizer
21310610	63	Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.	Theravance
20716489	12	FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.	University of Wuerzburg
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
20384344	42	Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.	Meiji Seika Kaisha
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
20137933	218	Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.	Amgen
20043678	92	Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.	Pfizer
20004578	28	Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.	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
19646865	45	Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.	Pfizer
19663387	29	Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.	Neurocrine Biosciences
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
18922694	84	Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.	Johnson & Johnson Prd
	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
19438238	45	Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.	Vanderbilt University Medical Center
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
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
18701276	97	Highly functionalized 7-azaindoles as selective PPAR gamma modulators.	Merck Research Laboratories
18621528	133	Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.	Pfizer
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
17398090	18	Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.	Ucb Pharma
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
16789729	25	A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.	Neurocrine Biosciences
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
16439121	46	First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.	Ucb Pharma
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
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
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
11708906	15	Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.	University of Bologna
11378358	254	Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands.	Columbia University College of Physicians and Surgeons
32122737	85	Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.	University of Chinese Academy of Sciences
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
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
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
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
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
10450976	1	Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.	Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories
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)
30554957	105	Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M	University of Kentucky
30605331	236	Design and in Vivo Characterization of A	Medical College of Wisconsin
31185168	144	Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.	Rti International
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
26565745	165	Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.	Janssen Pharmaceutica
24088171	19	Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.	Boehringer Ingelheim Pharma
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)
17084634	24	Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.	Universit£
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
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
29324345	122	Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.	Shanghai Institute of Materia Medica
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
29456793	72	Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.	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
1560441	35	Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).	Institute of Research
28442253	68	Optimization of M	Vanderbilt University Medical Center
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
22050606	36	a-Carbonic anhydrases are sulfatases with cyclic diol monosulfate esters.	Dumlupinar University
28160944	6	Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.	Jaipur National University
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
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
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
10421757	5	Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.	Institute of Genetics and Molecular and Cellular Biology (Igbmc)
19457661	21	Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.	Banyu Pharmaceutical
18247549	45	Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes.	Schering-Plough Research Institute
17451234	12	Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery.	Astex
12773052	14	Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.	Sapienza University of Rome
8494379	4	In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.	National Cancer Institute-Bethesda
15725032	3	Development of a technique to determine bicyclomycin-rho binding and stoichiometry by isothermal titration calorimetry and mass spectrometry.	University of North Carolina