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 |
| 27502700 |
36 |
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
Novartis Institutes of Biomedical Research (Nibr) |
| 27173801 |
29 |
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration. |
Vanderbilt University Medical Center |
| 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 |
| 26631313 |
20 |
Design and optimization of selective azaindole amide M1 positive allosteric modulators. |
Pfizer |
| 26428869 |
7 |
Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists. |
Sumitomo Dainippon Pharma |
| 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 |
| 26227772 |
22 |
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity. |
City University of New York |
| 26191365 |
49 |
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
Novartis Institutes For Biomedical Research |
| 26191354 |
20 |
Pyrrolopyridine or Pyrazolopyridine Derivatives. |
Temple University |
| 26112443 |
84 |
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414. |
Boehringer Ingelheim Pharma |
| 26077492 |
92 |
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition. |
Boehringer Ingelheim Pharma |
| 25893046 |
77 |
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5. |
Bristol-Myers Squibb |
| 25478907 |
29 |
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor. |
University of W£Rzburg |
| 25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
| 25800115 |
62 |
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists. |
RhôNe-Poulenc Rorer |
| 25765911 |
9 |
Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists. |
Korea Institute of Science and Technology |
| 24980056 |
44 |
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites. |
Universit£ |
| 24916029 |
42 |
Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Part 2. |
Astellas Pharma |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 24856064 |
9 |
Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists. |
Dainippon Sumitomo Pharma |
| 25435150 |
40 |
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators. |
Vanderbilt University Medical Center |
| 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 |
| 24856614 |
6 |
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M1 muscarinic acetylcholine receptor. |
Monash University (Parkville Campus) |
| 24852118 |
7 |
Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists. |
Dainippon Sumitomo Pharma |
| 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£ |
| 23416001 |
32 |
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. |
Vanderbilt University Medical Center |
| 24900656 |
9 |
Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists. |
Dainippon Sumitomo Pharma |
| 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 |
| 23237839 |
23 |
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. |
Vanderbilt University Medical Center |
| 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 |
| 17977730 |
42 |
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor. |
University of Minnesota |
| 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 |
| 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 |
| 22984902 |
59 |
Selective fluorescent nonpeptidic antagonists for vasopressin V2 GPCR: application to ligand screening and oligomerization assays. |
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£ |
| 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 |
| 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 |
| 20188547 |
152 |
Novel benzothiophene H1-antihistamines for the treatment of insomnia. |
Neurocrine Biosciences |
| 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 |
| 18485703 |
37 |
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors. |
Boehringer Ingelheim Pharma |
| 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£ |
| 16213721 |
60 |
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands. |
National Institute On Drug Abuse-Intramural Research Program |
| 16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
| 15294002 |
18 |
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor. |
Umr Cnrs/Ulp 7081 |
| 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 |
| 11170639 |
73 |
Current and novel approaches to the drug treatment of schizophrenia. |
Merck Sharp and Dohme Research Laboratories |
| 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 |
| 22177783 |
122 |
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
Argenta Discovery |
| 22245230 |
128 |
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
Florida A&M University |
| 22197142 |
42 |
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. |
Vanderbilt University Medical Center |
| 22153347 |
111 |
Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia. |
Neurocrine Biosciences |
| 22030026 |
13 |
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator. |
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 |
| 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 |
| 21615150 |
14 |
Progress in structure based drug design for G protein-coupled receptors. |
Heptares Therapeutics |
| 24900216 |
33 |
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands. |
TBA |
| 21524581 |
105 |
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists. |
RhôNe-Poulenc Rorer |
| 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 |
| 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 |
| 20347297 |
61 |
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia. |
Neurocrine Biosciences |
| 20227880 |
144 |
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia. |
Neurocrine Biosciences |
| 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 |
| 20156687 |
7 |
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
Vanderbilt University Medical Center |
| 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 |
| 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 |
| 19632840 |
43 |
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists. |
Tsukuba Research Institute |
| 19553115 |
96 |
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia. |
Neurocrine Biosciences |
| 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 |
| 19588934 |
71 |
Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships. |
Abbott Laboratories |
| 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 |
| | 14 |
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity |
TBA |
| | 31 |
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists |
TBA |
| | 24 |
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptors |
TBA |
| | 74 |
New indole derivatives as potent and selective serotonin uptake inhibitors |
TBA |
| | 45 |
SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndrome |
TBA |
| | 88 |
A rationale for the design and synthesis of m1 selective muscarinic agonists. |
TBA |
| | 40 |
Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5 |
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 |
| 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 |
| 18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
Amgen |
| 18595716 |
142 |
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
Florida A&M University |
| 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 |
| 18052023 |
30 |
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
Boehringer Ingelheim Pharma |
| 18032038 |
38 |
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives. |
Ucb Pharma |
| 17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
| 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 |
| 17448659 |
29 |
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists. |
Cerep |
| 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 |
| 16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
| 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 |
| 16302823 |
7 |
On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies. |
Umr Cnrs/Ulp 7081 |
| 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 |
| 15582404 |
68 |
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas. |
Astrazeneca |
| 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 |
| 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 |
| 12617901 |
23 |
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists. |
F. Hoffmann-La Roche |
| 12565973 |
33 |
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. |
Schering-Plough Research Institute |
| 11741475 |
56 |
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists. |
The University of Toledo |
| 11708906 |
15 |
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators. |
University of Bologna |
| 11597415 |
36 |
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands. |
Seoul National University |
| 11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College of Physicians and Surgeons |
| 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 |
| 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 |
| 32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
| 10522693 |
14 |
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors. |
Institute of Science and Technology |
| 31074983 |
202 |
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M |
University of Regensburg |
| 30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
University of North Carolina At Chapel Hill |
| 10377229 |
107 |
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
University of GöTeborg |
| 10206558 |
50 |
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists. |
Schering-Plough Research Institute |
| 30300845 |
43 |
1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio. |
Universit£ |
| 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 |
| 9464368 |
78 |
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists. |
Eli Lilly |
| 31401465 |
52 |
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands. |
Julius Maximilian University of W£Rzburg |
| 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 |
| 9406603 |
49 |
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
University of Groningen |
| 31613617 |
195 |
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
| 30827105 |
23 |
Fluorination of Photoswitchable Muscarinic Agonists Tunes Receptor Pharmacology and Photochromic Properties. |
Julius Maximilian University of W£Rzburg |
| 30106578 |
10 |
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
TBA |
| 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 |
| 24900754 |
2 |
Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1. |
Montclair State University |
| 23718562 |
3 |
Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. |
Monash University |
| 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£ |
| 17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
| 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£ |
| 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 |
| 30383372 |
190 |
Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
Huazhong University of Science and Technology |
| 30431269 |
41 |
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. |
Pfizer |
| 3712371 |
49 |
A novel class of conformationally restricted heterocyclic muscarinic agonists. |
TBA |
| 30258541 |
94 |
VU6007477, a Novel M |
Vanderbilt Univercity |
| 29716781 |
28 |
Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program. |
Pfizer |
| 29544056 |
3 |
Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M |
Monash University (Parkville Campus) |
| 29533874 |
76 |
The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
University of Defence |
| 29146472 |
71 |
Discovery of the first low-shift positive allosteric modulators for the muscarinic M1 receptor. |
Roche Pharma Research and Early Development |
| 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 |
| 29754948 |
69 |
The discovery of VU0486846: steep SAR from a series of M |
Vanderbilt University Medical Center |
| 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£ |
| 28958623 |
35 |
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H |
Glaxosmithkline |
| 28763213 |
193 |
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity. |
Jagiellonian University Medical College |
| 1674541 |
24 |
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity. |
Harvard Medical School |
| 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 |
| 28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
| 1433209 |
58 |
Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore. |
Eli Lilly |
| 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 |
| 28389149 |
56 |
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na |
Department of Discovery Chemistry Merck |
| 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 |
| 26851737 |
36 |
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies. |
University of Karachi |
| 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 |
| 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 |
| 9223589 |
17 |
N-(3-lodoprop-2E-enyl)-2beta-carbomethoxy-3beta-(3',4'-dichloro phenyl)nortropane (beta-CDIT), a tropane derivative: pharmacological characterization as a specific ligand for the dopamine transporter in the rodent brain. |
University of Tours |
| 7616416 |
11 |
7-(4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro-2(1H)-quinolinone (OPC-14597), a new putative antipsychotic drug with both presynaptic dopamine autoreceptor agonistic activity and postsynaptic D2 receptor antagonistic activity. |
Third Tokushima Institute of New Drug Research |
| 15006388 |
34 |
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents. |
Hoffmann-La Roche |
| 10956187 |
18 |
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. |
University of Newcastle |
| 12773052 |
14 |
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
Sapienza University of Rome |
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