136 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Cmpds
Data
Article Title
Organization
26
Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits.
Pfizer
60
A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
Harvard Medical School
2
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Bristol Myers Squibb
65
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups.
Actelion Pharmaceuticals
25
Novel S1P1 receptor agonists - Part 5: From amino-to alkoxy-pyridines.
Actelion Pharmaceuticals
19
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Bristol Myers Squibb
6
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Bristol Myers Squibb
6
Synthesis, identification, and biological activity of metabolites of two novel selective S1P1 agonists.
Peking Union Medical College
38
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Glaxosmithkline
19
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
55
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Boehringer Ingelheim Pharmaceuticals
1
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.
Glaxosmithkline
14
Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
25
Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
32
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Arena Pharmaceuticals
36
Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
Peking Union Medical College
9
Synthesis and SAR studies of benzyl ether derivatives as potent orally active S1P1 agonists.
Daiichi Sankyo
11
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Arena Pharmaceuticals
19
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
39
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Glaxosmithkline
33
Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists.
Boehringer Ingelheim Pharmaceuticals
31
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Genomics Institute of The Novartis Research Foundation
11
Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1.
Praecis Pharmaceuticals Incorporated (Currently Glaxosmithkline)
31
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.
Glaxosmithkline
23
Discovery of a novel class of zwitterionic, potent, selective and orally active S1P1 direct agonists.
RhôNe-Poulenc Rorer
7
An oral sphingosine 1-phosphate receptor 1 (S1P(1)) antagonist prodrug with efficacy in vivo: discovery, synthesis, and evaluation.
Novartis Pharma
10
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Glaxosmithkline
12
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.
Arena Pharmaceuticals
17
Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.
TBA
34
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
Glaxosmithkline
25
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P3-sparing S1P1 agonists.
Daiichi Sankyo
37
Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.
Exelixis
10
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
TBA
42
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Glaxosmithkline
6
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
University of Montreal
11
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
University of Virginia
8
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
University of Virginia
19
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
26
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Merck Research Laboratories
12
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
University of Virginia
3
Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
Daiichi Sankyo
32
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
Daiichi Sankyo
26
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups.
Amgen
20
Quinolinone-based agonists of S1P¿?: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Amgen
17
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P¿? agonists with in vivo lymphocyte-depleting activity.
Amgen
13
Structure-activity relationship studies of S1P agonists with a dihydronaphthalene scaffold.
Ono Pharmaceutical
7
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
Institute of Pharmacology & Toxicology
41
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
9
Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.
Glaxosmithkline
10
SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor.
The Scripps Research Institute
41
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
The Scripps Research Institute
11
Structure-activity relationship studies of sphingosine-1-phosphate receptor agonists with N-cinnamyl-ß-alanine moiety.
Ono Pharmaceutical
23
Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)
TBA
26
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS
TBA
69
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Actelion Pharmaceuticals
20
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
15
Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
8
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
11
S1P receptor mediated activity of FTY720 phosphate mimics.
Novartis Institutes For Biomedical Research
15
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
Novartis Institutes For Biomedical Research
20
Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
6
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
Praecis Pharmaceuticals
15
Pharmacophore-based design of sphingosine 1-phosphate-3 receptor antagonists that include a 3,4-dialkoxybenzophenone scaffold.
Toa Eiyo
12
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
University of Virginia
28
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
41
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Merck
11
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
11
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Merck Research Laboratories
65
Discovery of Novel Sphingosine-1-Phosphate-1 Receptor Agonists for the Treatment of Multiple Sclerosis.
Korea Institute of Science & Technology (Kist)
4
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
30
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
Washington University
41
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.
Ocean University of China
23
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Merck Research Laboratories
28
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Merck Research Laboratories
12
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Merck Research Laboratories
4
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
13
Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design.
TBA
4
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
21
Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1).
University of Dundee
34
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol Myers Squibb
28
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Bristol Myers Squibb
29
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.
Washington University
55
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
54
Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines.
Actelion Pharmaceuticals
54
Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes.
Actelion Pharmaceuticals
3
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
Praecis Pharmaceuticals
28
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
The Scripps Research Institute
5
NBD-labeled derivatives of the immunomodulatory drug FTY720 as tools for metabolism and mode of action studies.
Novartis Institutes For Biomedical Research
22
Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P
Ono Pharmaceutical
17
Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol Myers Squibb
366
Sphinogosine-1 -phosphate receptor modulators for treatment of cardiopulmonary disorders
The Scripps Research Institute
58
Compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof
Washington University
365
Sphinogosine-1-phosphate receptor modulators for treatment of cardiopulmonary disorders
The Scripps Research Institute
153
6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
Merck Serono
154
6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
Allergan
182
Inhibitors of gas for treating autoinflammatory diseases and cancer metastasis
The Rockefeller University; Memorial Sloan-Kettering Cancer Center
4
Benzoimidazole derivatives as anticancer agents
Centre Leon Berard; Hospices Civils De Lyon; Universite Claude Bernard Lyon 1; Centre National De La Recherche Scientifique; Institut National De La Sante Et De La Recherche Medicale (Inserm)
448
ALPHA PROTEIN KINASE 1 INHIBITORS FOR USE IN TREATING KIDNEY DISEASES AND KIDNEY-RELATED DISEASES
Shanghai Yao Yuan Biotechnology Co.
4
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
Mitsubishi Pharma
8
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
Merck Research Laboratories