136 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
Pfizer
A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
Harvard Medical School
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Bristol-Myers Squibb
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups.
Actelion Pharmaceuticals
Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines.
Actelion Pharmaceuticals
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Bristol-Myers Squibb Research and Development
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Bristol-Myers Squibb Research and Development
Synthesis, identification, and biological activity of metabolites of two novel selective S1P1 agonists.
Peking Union Medical College
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Glaxosmithkline
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.
Glaxosmithkline
Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Arena Pharmaceuticals
Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
Peking Union Medical College
Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P1 agonists.
Daiichi Sankyo
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Arena Pharmaceuticals
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Glaxosmithkline
Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Genomics Institute of The Novartis Research Foundation
Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.
Praecis Pharmaceuticals Incorporated (Currently Glaxosmithkline)
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.
Glaxosmithkline
Discovery of a novel class of zwitterionic, potent, selective and orally active S1P1 direct agonists.
RhôNe-Poulenc Rorer
An oral sphingosine 1-phosphate receptor 1 (S1P(1)) antagonist prodrug with efficacy in vivo: discovery, synthesis, and evaluation.
Novartis Pharma
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Glaxosmithkline
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.
Arena Pharmaceuticals
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
Glaxosmithkline
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P3-sparing S1P1 agonists.
Daiichi Sankyo
Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.
Exelixis
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
TBA
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Glaxosmithkline
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
University of Montreal
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
University of Virginia
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
University of Virginia
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Merck Research Laboratories
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
University of Virginia
Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
Daiichi Sankyo
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
Daiichi Sankyo
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups.
Amgen
Quinolinone-based agonists of S1P¿?: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Amgen
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P¿? agonists with in vivo lymphocyte-depleting activity.
Amgen
Structure-activity relationship studies of S1P agonists with a dihydronaphthalene scaffold.
Ono Pharmaceutical
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
Institute of Pharmacology & Toxicology
Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P¿? agonists.
Arena Pharmaceuticals
Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.
Glaxosmithkline
SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor.
The Scripps Research Institute
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
The Scripps Research Institute
Structure-activity relationship studies of sphingosine-1-phosphate receptor agonists with N-cinnamyl-ß-alanine moiety.
Ono Pharmaceutical
Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)
TBA
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS
TBA
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Actelion Pharmaceuticals
Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
Mitsubishi Tanabe Pharma
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
S1P receptor mediated activity of FTY720 phosphate mimics.
Novartis Institutes For Biomedical Research
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
Novartis Institutes For Biomedical Research
Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
Pharmacophore-based design of sphingosine 1-phosphate-3 receptor antagonists that include a 3,4-dialkoxybenzophenone scaffold.
Toa Eiyo
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
University of Virginia
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Merck Research Laboratories
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Merck
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Merck Research Laboratories
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
Korea Institute of Science & Technology (Kist)
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Novartis Institutes For Biomedical Research
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
Washington University
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.
Ocean University of China
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Merck Research Laboratories
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Merck Research Laboratories
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Merck Research Laboratories
Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb Research and Development
Bicyclic Ligand-Biased Agonists of S1P
Bristol Myers Squibb Research & Early Development
Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design.
TBA
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P
Bristol-Myers Squibb
Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1).
University of Dundee
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Bristol-Myers Squibb
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.
Washington University
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Abbvie Bioresearch Center
Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines.
Actelion Pharmaceuticals
Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes.
Actelion Pharmaceuticals
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
Praecis Pharmaceuticals
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
The Scripps Research Institute
NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies.
Novartis Institutes For Biomedical Research
Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P
Ono Pharmaceutical
Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb
DENDRIMER COMPOSITIONS AND METHODS FOR DRUG DELIVERY TO THE EYE
Ashvattha Therapeutics
6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR
Blueprint Medicines
Substituted benzimidazoles, their preparation and their use as pharmaceuticals
Neomed Institute
Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
Chong Kun Dang Pharmaceutical
The SAMPL4 host-guest blind prediction challenge: an overview.
University of California San Diego
Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
Astrazeneca
Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives.
Bezmialem Vakif University
N1-(3-cyclohexylbutanoyl)-N2-[3-(1H-imidazol-4-yl)propyl]guanidine (UR-AK57), a potent partial agonist for the human histamine H1- and H2-receptors.
University of Kansas
New active HIV-1 protease inhibitors derived from 3-hexanol: conformation study of the free inhibitors in crystalline state and in complex with the enzyme.
Technical University of LÓDz
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization.
Merck Research Laboratories
Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes.
Bristol-Myers Squibb
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Bristol-Myers Squibb
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists.
Johnson & Johnson Pharmaceutical
Inhibitor binding in a class 2 dihydroorotate dehydrogenase causes variations in the membrane-associated N-terminal domain.
University of Copenhagen
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.
Purdue University
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight.
Abbott Bioresearch Center