The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 12467617 |
17 |
New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. |
Meiji Seika Kaisha |
| 12392747 |
36 |
SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties. |
Glaxosmithkline |
| 11992776 |
70 |
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists. |
Glaxosmithkline |
| 11266169 |
27 |
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor. |
Smithkline Beecham Pharmaceuticals |
| 11597412 |
116 |
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor. |
Glaxosmithkline |
| 27908761 |
55 |
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. |
Eli Lilly |
| 27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
| 26700945 |
68 |
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. |
National Institute of Biological Sciences, Beijing |
| 26852005 |
82 |
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists. |
Yonsei University |
| 26739781 |
237 |
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines. |
The Alexander Shulgin Research Institute |
| 26475518 |
19 |
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor. |
City University of New York |
| 26200936 |
39 |
Applications of Fluorine in Medicinal Chemistry. |
Bristol-Myers Squibb Research and Development |
| 26227772 |
22 |
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity. |
City University of New York |
| 25127461 |
36 |
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression. |
Yonsei University |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 24878222 |
50 |
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors. |
Pfizer |
| 16730983 |
165 |
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: synthesis and biological evaluation. |
Glaxosmithkline |
| 23477943 |
51 |
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression. |
Bristol-Myers Squibb |
| 23218776 |
45 |
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands. |
H. Lundbeck |
| 20951584 |
105 |
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3. |
Glaxosmithkline |
| 19071020 |
66 |
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II. |
Glaxosmithkline |
| 19286377 |
101 |
8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II. |
Glaxosmithkline |
| 18799312 |
84 |
6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
| 19146417 |
70 |
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor. |
Glaxosmithkline |
| 18829312 |
64 |
Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity. |
Glaxosmithkline |
| 18433113 |
124 |
Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
Glaxosmithkline |
| 16039851 |
57 |
8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands. |
Glaxosmithkline |
| 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 |
| 11229746 |
6 |
First tricyclic oximino derivatives as 5-HT3 ligands. |
Universit£ |
| 11140733 |
92 |
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134). |
Smithkline Beecham Pharmaceuticals |
| 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 |
| 23102207 |
122 |
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers. |
Universit£ |
| 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 |
| 21726069 |
98 |
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
University of Namur |
| 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 |
| 20727749 |
17 |
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). |
University of Sydney |
| 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 |
| 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 |
| 16480278 |
279 |
1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. |
Organix |
| 16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
| 16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
| 15658848 |
103 |
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. |
Wyeth Research |
| 12519065 |
243 |
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
H. Lundbeck |
| 12954071 |
109 |
A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. |
Alcon Research |
| 11708905 |
20 |
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy. |
Eli Lilly |
| 11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
| 9435911 |
36 |
2-(1-Naphthyloxy)ethylamines with enhanced affinity for human 5-HT1D beta (h5-HT1B) serotonin receptors. |
Medical College of Virginia/Virginia Commonwealth University |
| 7658447 |
72 |
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. |
Centre De Recherche Pierre Fabre |
| 7783153 |
189 |
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 2. Effects of 8-amino nitrogen substitution on serotonin receptor binding and pharmacology. |
Upjohn Laboratories |
| 2213824 |
20 |
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists. |
Pfizer |
| 15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
| 15109634 |
129 |
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis. |
Eli Lilly |
| 21982496 |
4 |
A novel potential therapeutic avenue for autism: design, synthesis and pharmacophore generation of SSRIs with dual action. |
Qatar University |
| 21958544 |
31 |
Indolin-2-one p38a inhibitors III: bioisosteric amide replacement. |
RhôNe-Poulenc Rorer |
| 21520940 |
40 |
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. |
Vu University Medical Center |
| 21093272 |
126 |
Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists. |
Wyeth Research |
| 20949929 |
63 |
Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. |
Bristol-Myers Squibb |
| 20932009 |
127 |
5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists. |
Wyeth Research |
| 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 |
| 20170099 |
58 |
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. |
Wyeth Research |
| 20088516 |
7 |
De novo design of a picomolar nonbasic 5-HT(1B) receptor antagonist. |
Astrazeneca Pharmaceuticals |
| 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 |
| | 45 |
Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B 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 |
| 18557608 |
108 |
Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors. |
Wyeth Research |
| 18511284 |
64 |
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor. |
Wyeth Research |
| 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 |
| 18378462 |
5 |
Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents. |
Sinhgad College of Pharmacy |
| 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 |
| 17434731 |
51 |
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors. |
Eli Lilly |
| 17257843 |
35 |
A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening. |
Pfizer |
| 17126021 |
12 |
Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides: a late-stage diversification approach to potent 5HT1B antagonists. |
Astrazeneca 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 |
| 16392816 |
113 |
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. |
Alcon Research |
| 16361098 |
70 |
Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists. |
F. Hoffmann-La Roche |
| 16219465 |
82 |
Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs. |
Abbott |
| 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 |
| 16055331 |
45 |
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. |
Carlsson Research |
| 15546719 |
38 |
Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists. |
Eli Lilly |
| 15324890 |
29 |
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. |
Virginia Commonwealth University |
| 14741277 |
44 |
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands. |
Nps Pharmaceuticals |
| 14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
| 14505640 |
38 |
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands. |
Nps Pharmaceuticals |
| 12825944 |
184 |
Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides. |
Eli Lilly |
| 12643910 |
55 |
Identification of a novel series of selective 5-HT7 receptor antagonists. |
Glaxosmithkline |
| 11689074 |
112 |
N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands. |
Merck Sharp & Dohme Research Laboratories |
| 11514164 |
36 |
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists. |
Glaxosmithkline |
| 11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College of Physicians and Surgeons |
| 32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
| 11055342 |
21 |
N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. |
Virginia Commonwealth University |
| 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 |
| 10937729 |
21 |
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists. |
Nps Allelix |
| 10853656 |
24 |
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine. |
Nps Allelix |
| 10612601 |
30 |
4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine. |
Merck Sharp & Dohme Research Laboratories |
| 10585208 |
212 |
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. |
Merck Sharp & Dohme Research Laboratories |
| 32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
| 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 |
| 10377215 |
104 |
Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles. |
Merck Sharp & Dohme Research Laboratories |
| 10052976 |
126 |
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents. |
Merck Sharp and Dohme Research Laboratories |
| 10052975 |
129 |
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor. |
Merck Sharp and Dohme Research Laboratories |
| 9986723 |
29 |
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. |
Eli Lilly |
| 29400967 |
136 |
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
Bristol-Myers Squibb |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 9871775 |
29 |
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
Centre De Recherche Pierre Fabre |
| 9871581 |
12 |
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist. |
Centre De Recherche Pierre Fabre |
| 9857099 |
94 |
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia. |
Synaptic Pharmaceutical |
| 9632357 |
59 |
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. |
Virginia Commonwealth University |
| 9397179 |
40 |
5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. |
Centre De Recherche Pierre Fabre |
| 9357521 |
20 |
Differentiation between partial agonists and neutral 5-HT1B antagonists by chemical modulation of 3-[3-(N,N-dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562). |
Centre De Recherche Pierre Fabre |
| 9357515 |
55 |
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. |
Merck Sharp and Dohme Research Laboratories |
| 9357514 |
55 |
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype. |
Merck Sharp and Dohme Research Laboratories |
| 8960551 |
74 |
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists. |
Centre De Recherche Pierre Fabre |
| 8941384 |
51 |
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
University of Groningen |
| 31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
| 8568822 |
80 |
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors. |
Virginia Commonwealth University |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 8071931 |
20 |
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. |
Medical College of Virginia/Virginia Commonwealth University |
| 7783152 |
170 |
Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
GöTeborg University |
| 7658443 |
5 |
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties. |
Wellcome Research Laboratories |
| 21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
| 18316188 |
31 |
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation. |
Glaxosmithkline |
| 17942309 |
18 |
Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification. |
Glaxosmithkline |
| 17129726 |
121 |
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors. |
Glaxosmithkline |
| 16337790 |
53 |
Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands. |
Merck Sharp and Dohme Research Laboratories |
| 16153839 |
64 |
Identification of a potent and selective 5-HT1B receptor antagonist. |
Glaxosmithkline |
| 15887956 |
77 |
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. |
Glaxosmithkline |
| 16002289 |
65 |
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. |
Glaxosmithkline |
| 14613313 |
34 |
A novel ergot alkaloid as a 5-HT(1A) inhibitor produced by Dicyma sp. |
Glaxosmithkline R&D |
| 11262079 |
57 |
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation. |
Glaxowellcome |
| 30028132 |
135 |
Discovery of ?-Arrestin Biased Ligands of 5-HT |
Korea Institute of Science and Technology |
| 28745513 |
309 |
Modulating the Serotonin Receptor Spectrum of Pulicatin Natural Products. |
University of The Philippines |
| 29029933 |
45 |
Highly potent and selective Na |
Pfizer |
| 29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
| 2374139 |
50 |
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole. |
Pfizer |
| 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 |
| 1447752 |
28 |
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin. |
Pfizer |
| 28485934 |
48 |
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors. |
Astrazeneca |
| 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 |
| 26943478 |
16 |
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
Chulabhorn Research Institute |
| 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 |
| 26364932 |
22 |
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity. |
University of North Carolina At Chapel Hill |
| 8386236 |
11 |
In vitro and in vivo pharmacological characterization of N6-cyclopentyl-9-methyladenine (N-0840): a selective, orally active A1 adenosine receptor antagonist. |
Whitby Research |
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