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 |
| 12372505 |
120 |
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands. |
Abbott Laboratories |
| 12113835 |
176 |
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1. |
Abbott Laboratories |
| 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 |
| 27866818 |
84 |
The discovery of quinoline based single-ligand human H |
Glaxosmithkline |
| 27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
| 27643714 |
26 |
Identification of Ligand Binding Hot Spots of the Histamine H |
Vrije Universiteit Amsterdam |
| 27717652 |
275 |
Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors. |
Florida A&M University |
| 27364609 |
230 |
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores. |
Florida A&M University |
| 27312422 |
219 |
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. |
Florida A&M University |
| 27173799 |
97 |
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics. |
Shanghai Institute of Materia Medica |
| 27007611 |
115 |
Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
University of Regensburg |
| 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 |
| 26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
| 26718844 |
55 |
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity. |
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg |
| 25993395 |
19 |
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators. |
Janssen Research and Development |
| 26191365 |
49 |
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. |
Novartis Institutes For Biomedical Research |
| 25494650 |
8 |
CNS drug design: balancing physicochemical properties for optimal brain exposure. |
Eli Lilly |
| 25827402 |
54 |
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity. |
Teva Global R & D. |
| 25557493 |
109 |
Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
Jagiellonian University Collegium Medicum |
| 25070422 |
126 |
Further evaluation of the tropane analogs of haloperidol. |
Florida A&M University |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 25343529 |
221 |
Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
Universit£ |
| 25318072 |
48 |
Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2. |
Max Planck Institute of Psychiatry |
| 24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
| 24800940 |
146 |
Identification of a new selective dopamine D4 receptor ligand. |
Florida A&M University |
| 24690494 |
92 |
Antagonists of the kappa opioid receptor. |
The Scripps Research Institute |
| 24559051 |
141 |
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
Intra-Cellular Therapies |
| 24650714 |
21 |
Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties. |
United Arab Emirates University |
| 24365159 |
35 |
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
University of Missouri |
| 24900633 |
11 |
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors. |
Amgen |
| 24269482 |
35 |
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. |
Glaxosmithkline |
| 24161834 |
17 |
The discovery of the benzazepine class of histamine H3 receptor antagonists. |
Glaxosmithkline |
| 24147864 |
6 |
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1). |
National Institute of Mental Health |
| 23919353 |
8 |
Polypharmacology - foe or friend? |
F. Hoffmann-La Roche |
| 24454993 |
1 |
Discovery of?2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor. |
University of Dundee |
| 24035337 |
10 |
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character. |
Virginia Commonwealth University |
| 23981939 |
32 |
N-substituted 8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes ass receptor ligands with potential neuroprotective effects. |
The University of Sydney |
| 24611085 |
101 |
Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor. |
Sanford-Burnham Medical Research Institute |
| 23816046 |
8 |
Synthesis and in vivo evaluation of [(18)F]2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)-dione ([(18)F]FECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates. |
Columbia University Medical Center |
| 23707254 |
7 |
Selectivity of phenothiazine cholinesterase inhibitors for neurotransmitter systems. |
Dalhousie University |
| 23602445 |
23 |
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. |
Ucl School of Pharmacy |
| 23591112 |
4 |
Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II). |
Sanofi Us |
| 23582449 |
20 |
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
Institute of Organic Synthesis |
| 23466604 |
36 |
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
Universit£ |
| 23403082 |
28 |
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
Broad Institute of Mit and Harvard |
| 23558237 |
17 |
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787. |
Griffin Discoveries |
| 24900647 |
8 |
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand. |
Goethe University |
| 14667234 |
23 |
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists. |
Vrije Universiteit Amsterdam |
| 12443779 |
44 |
2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties. |
Janssen-Cilag |
| 21944853 |
41 |
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R. |
University of Regensburg |
| 20674357 |
66 |
Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders. |
Glaxosmithkline |
| 16408006 |
3 |
Linking agonist binding to histamine H1 receptor activation. |
Vrije Universiteit Amsterdam |
| 20409707 |
66 |
Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity. |
University of Regensburg |
| 19791743 |
41 |
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. |
University of Regensburg |
| 19524331 |
33 |
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines. |
Johnson & Johnson Pharmaceutical Research & Development |
| 19317445 |
53 |
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
University of Regensburg |
| 19053770 |
68 |
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. |
Vrije Universiteit Amsterdam |
| 18248991 |
323 |
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems. |
Glaxosmithkline |
| 12657274 |
109 |
Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists. |
Abbott Laboratories |
| 11755365 |
113 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2. |
Janssen-Cilag |
| 11755364 |
104 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1. |
Janssen-Cilag |
| 12113836 |
162 |
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs. |
Abbott Laboratories |
| 23142617 |
57 |
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I. |
Astrazeneca |
| 23116889 |
88 |
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: optimising in vivo clearance. |
Astrazeneca |
| 23099096 |
88 |
Novel azulene derivatives for the treatment of erectile dysfunction. |
Friedrich-Alexander University |
| 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 |
| 21486038 |
177 |
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. |
H. Lundbeck |
| 23641311 |
38 |
From a4ß2 Nicotinic Ligands to the Discovery of s1 Receptor Ligands: Pharmacophore Analysis and Rational Design. |
TBA |
| 23009245 |
53 |
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. |
Sanford-Burnham Medical Research Institute |
| 23006002 |
35 |
Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists. |
Suven Life Sciences |
| 22931505 |
69 |
Chemokine receptor antagonists. |
National Heart and Lung Institute |
| 23031591 |
90 |
The discovery of CCR3/H1 dual antagonists with reduced hERG risk. |
Astrazeneca |
| 22793499 |
19 |
Shape-based reprofiling of FDA-approved drugs for the H1 histamine receptor. |
University of Oxford |
| 22694093 |
16 |
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. |
National Institute of Biological Sciences |
| 23021991 |
153 |
Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092. |
Astrazeneca |
| 21062081 |
47 |
Histamine H3 receptor as a drug discovery target. |
TBA |
| 22985961 |
99 |
Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists. |
Glaxosmithkline |
| 22578490 |
35 |
Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists. |
Cephalon |
| 22520153 |
135 |
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants. |
Florida A&M University |
| 22313242 |
146 |
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. |
Pfizer |
| 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 |
| 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 |
| 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 |
| 20541426 |
46 |
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor. |
Meiji Seika Kaisha |
| 20299215 |
49 |
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. |
Argenta Discovery |
| 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 |
| 17846138 |
26 |
Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
Veterans Affairs Medical Center |
| 19091563 |
79 |
Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
Johann Wolfgang Goethe Universit£T |
| 18950149 |
75 |
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists. |
University of Regensburg |
| 16562853 |
22 |
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro. |
Tom'S of Maine |
| 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 |
| 17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
| 18077160 |
126 |
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series. |
Abbott Laboratories |
| 18023344 |
77 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. |
F. Hoffmann-La Roche |
| 17998160 |
101 |
Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. |
F. Hoffmann-La Roche |
| 17407815 |
27 |
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. |
Janssen-Cilag |
| 16821797 |
21 |
(R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties. |
Mitsubishi Pharma |
| 16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
| 15771458 |
5 |
Norpiperidine imidazoazepines as a new class of potent, selective, and nonsedative H1 antihistamines. |
Johnson & Johnson Pharmaceutical Research & Development |
| 14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
| 12747773 |
13 |
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior. |
Aventis Pharmaceuticals |
| 12213075 |
70 |
Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). |
Purdue University |
| 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 |
| 15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
| | 52 |
Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity |
TBA |
| | 24 |
1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists |
TBA |
| 22336245 |
72 |
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol. |
Florida A&M University |
| 22245230 |
128 |
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
Florida A&M University |
| 22153663 |
59 |
Ligand based design of novel histamine H4 receptor antagonists; fragment optimization and analysis of binding kinetics. |
Griffin Discoveries |
| 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 |
| 22153342 |
60 |
Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists. |
Cephalon |
| 22014551 |
33 |
Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists. |
Cephalon |
| 22007643 |
25 |
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor. |
Vu University Amsterdam |
| 21955944 |
39 |
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR). |
Pfizer |
| 21788137 |
33 |
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands. |
The University of Sydney |
| 20800486 |
16 |
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia. |
Neurocrine Biosciences |
| 19443217 |
60 |
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists. |
Chemical Diversity Research Institute |
| 21555222 |
25 |
Molecular hybridization of 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecane-3-ol with sigma (s) receptor ligands modulates off-target activity and subtype selectivity. |
The University of Sydney |
| 21470866 |
21 |
Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines. |
Dainippon Sumitomo Pharma |
| 21381763 |
52 |
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. |
Glaxosmithkline |
| 21232954 |
75 |
Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6. |
Neurocrine Biosciences |
| 21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
The University of Sydney |
| 20942472 |
88 |
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders. |
Glaxosmithkline |
| 20857909 |
176 |
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors. |
University of Copenhagen |
| 20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
| 20690643 |
68 |
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain. |
Meiji Seika Kaisha |
| 20667729 |
86 |
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists. |
Evotec (Uk) |
| 20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
| 20452213 |
65 |
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands. |
Johnson & Johnson Pharmaceutical Research & Development |
| 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 |
| 20153647 |
6 |
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure. |
Glaxosmithkline |
| 19786348 |
261 |
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists. |
F. Hoffmann-La Roche |
| 20045641 |
9 |
9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites. |
Virginia Commonwealth University |
| 20170186 |
49 |
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors. |
Glaxosmithkline |
| 19945877 |
50 |
Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. |
Chemical Diversity Research Institute |
| 19773175 |
41 |
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
Johann Wolfgang Goethe University |
| 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 |
| 19773162 |
72 |
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. |
Arena Pharmaceuticals |
| 19660947 |
24 |
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs. |
The Schering Plough Research Institute |
| 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 |
| 19520574 |
49 |
Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists. |
Tsukuba Research Institute |
| 19362477 |
24 |
Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists. |
Dainippon Sumitomo Phrama. |
| 19553110 |
16 |
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies. |
Tsukuba Research Institute |
| 8496700 |
16 |
The Role of Receptor Binding in Drug Discovery |
TBA |
| | 76 |
Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activity |
TBA |
| | 32 |
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) |
TBA |
| | 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
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 |
| 19329329 |
183 |
Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET. |
Institute of Nuclear Chemistry Johannes Gutenberg-University Mainz |
| 18952421 |
60 |
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18841880 |
82 |
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18817368 |
57 |
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. |
Merck Research Laboratories |
| 18783208 |
11 |
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function. |
National Institute of Mental Health |
| 18768318 |
37 |
Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
Amgen |
| 18598020 |
75 |
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. |
Tsukuba Research Institute |
| 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 |
| 18020391 |
12 |
From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling. |
F. Hoffmann-La Roche |
| 18020390 |
37 |
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach. |
F. Hoffmann-La Roche |
| 17976986 |
80 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
Pfizer |
| 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 |
| 17524641 |
69 |
3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists. |
Glaxosmithkline |
| 16942032 |
64 |
Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
Hokkaido University |
| 16621538 |
35 |
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol. |
Florida A&M University |
| 16458504 |
37 |
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand. |
Columbia University College of Physicians and Surgeons |
| 16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College of Physicians and Surgeons |
| 16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College of Physicians and Surgeons |
| 16134937 |
154 |
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. |
7Tm Pharma |
| 15771448 |
187 |
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. |
Janssen-Cilag |
| 15771415 |
155 |
Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
Johnson & Johnson Pharmaceutical Research & Development |
| 15686917 |
21 |
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds. |
Ucb Pharma |
| 15634025 |
29 |
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. |
Novo Nordisk |
| 15482930 |
22 |
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. |
Ucb Pharma |
| 15125929 |
66 |
Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. |
Janssen-Cilag |
| 15081022 |
20 |
5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity. |
Ucb Pharma |
| 14741266 |
203 |
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists. |
Abbott Laboratories |
| 12798320 |
64 |
A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines. |
Abbott Laboratories |
| 12723960 |
58 |
Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure. |
Hokkaido University |
| 12372500 |
108 |
Synthesis and evaluation of potent pyrrolidine H(3) antagonists. |
Abbott Laboratories |
| 11784148 |
81 |
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1. |
Pharmazeutisches Institut Der UniversitäT Freiburg |
| 32462865 |
26 |
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H |
Pfizer |
| 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 |
| 32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
| 32420741 |
134 |
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H |
University of Regensburg |
| 28797771 |
31 |
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H |
Jagiellonian University Medical College |
| 10956183 |
19 |
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability. |
Synaptic Pharmaceutical |
| 10937710 |
81 |
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones. |
Merck |
| 27331270 |
54 |
Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 31679973 |
18 |
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H |
China Pharmaceutical University |
| 32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
| 31421966 |
20 |
Rasagiline derivatives combined with histamine H |
Heinrich Heine University D£Sseldorf |
| 31021617 |
136 |
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D |
University of Pennsylvania |
| 30875219 |
254 |
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D |
University of North Carolina At Chapel Hill |
| 30605331 |
236 |
Design and in Vivo Characterization of A |
Medical College of Wisconsin |
| 31274307 |
24 |
Route to Prolonged Residence Time at the Histamine H |
Vu University Amsterdam |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 9857099 |
94 |
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. |
Synaptic Pharmaceutical |
| 31913038 |
13 |
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity. |
University of Florida |
| 31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
| 21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
| 21044842 |
206 |
Histamine H4 receptor agonists. |
University of Regensburg |
| 18357976 |
53 |
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. |
Vrije Universiteit Amsterdam |
| 15771452 |
49 |
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist. |
Vrije Universiteit Amsterdam |
| 12593665 |
188 |
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. |
Johannes Gutenberg-University of Mainz |
| 30431269 |
41 |
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. |
Pfizer |
| 30389290 |
146 |
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. |
Texas Tech University Health Sciences Center |
| 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 |
| 29730027 |
99 |
Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system. |
Jagiellonian University Medical College |
| 29395980 |
84 |
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs. |
University of Chinese Academy of Sciences |
| 29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
| 29990431 |
138 |
Selectivity Challenges in Docking Screens for GPCR Targets and Antitargets. |
University of California San Francisco |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 28774576 |
134 |
Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics. |
Xinjiang Technical Institute of Physics and Chemistry |
| 28776992 |
110 |
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors. |
Northwestern University |
| 28489950 |
119 |
Return of D |
University of Nebraska Medical Center |
| 1681106 |
27 |
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds. |
Pfizer |
| 27666135 |
59 |
Rapid synthesis of flavone-based monoamine oxidase (MAO) inhibitors targeting two active sites using click chemistry. |
Zhejiang University of Technology |
| 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 |
| 26518975 |
9 |
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues. |
Peking University |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
| 25462626 |
6 |
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes. |
Comsats Institute of Information Technology |
| 12388666 |
301 |
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. |
Institut De Recherches Servier |
| 7925364 |
13 |
Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene. |
UniversitÉ |
| 3828800 |
17 |
The characterization of [3H]sulpiride binding sites in rat striatal membranes. |
St, Marianna University School of Medicine |
| 17536795 |
118 |
Thiophene-anthranilamides as highly potent and orally available factor xa inhibitors |
Berlex Biosciences |
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