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 |
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 |
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 |
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 |
| 31 |
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists |
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 |
16439121 |
46 |
First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives. |
Ucb Pharma |
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 |
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£ |
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 |
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 |
29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
29456793 |
72 |
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains. |
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£ |
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 |