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Quinolinone-based agonists of S1P1: Use of a N-scan SAR strategy to optimize in vitro and in vivo activity

Author
PENNINGTON, Lewis D1 ; CROGHAN, Michael D1 ; MCELVAIN, Michele3 ; YANG XU4 ; XUXIA ZHANG5 ; FIORINO, Michael5 ; HORNER, Michelle6 ; MORRISON, Henry G7 ; ARNETT, Heather A5 ; FOTSCH, Christopher1 ; TASKER, Andrew S1 ; MIN WONG5 ; SHAM, Kelvin K. C1 ; CEE, Victor J1 ; PICKRELL, Alexander J1 ; HARRINGTON, Paul E1 ; FROHN, Michael J1 ; LANMAN, Brian A1 ; REED, Anthony B1 ; LEE, Matthew R2 ; HAN XU3
[1] Medicinal Chemistry, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[2] Molecular Structure, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[3] HTS and Molecular Pharmacology, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[4] Pharmacokinetics and Drug Metabolism, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[5] Inflammation Research, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[6] Toxicology, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
[7] Pharmaceutics, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, United States
Source

Bioorganic & medicinal chemistry letters (Print). 2012, Vol 22, Num 1, pp 527-531, 5 p

ISSN
0960-894X
Scientific domain
Biochemistry, molecular biology, biophysics; Pharmacology drugs
Publisher
Elsevier, Amsterdam
Publication country
Netherlands
Document type
Article
Language
English
Author keyword
Immunosuppression Multiple sclerosis N-scan SAR Physicochemical properties Sphingosine-1-phosphate-1 receptor agonist
Keyword (fr)
Agoniste Dérivé de la quinolone Dérivé de la quinoléine Immunodépression In vitro In vivo Propriété physicochimique Relation structure activité Récepteur biologique Sclérose en plaques Sphingosine-1-phosphate Récepteur sphingosine 1 phosphate Maladie inflammatoire Pathologie du système nerveux central Pathologie du système nerveux
Keyword (en)
Agonist Quinolone derivatives Quinoline derivatives Immunosuppression In vitro In vivo Physicochemical properties Structure activity relation Biological receptor Multiple sclerosis Sphingosine-1-phosphate Inflammatory disease Central nervous system disease Nervous system diseases
Keyword (es)
Agonista Quinolone derivado Quinolina derivado Inmunodepresión In vitro In vivo Propiedad fisicoquímica Relación estructura actividad Receptor biológico Esclerosis en placa Esfingosina-1-fosfato Enfermedad inflamatoria Sistema nervosio central patología Sistema nervioso patología
Classification
Pascal
002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments

Discipline
General pharmacology
Origin
Inist-CNRS
Database
PASCAL
INIST identifier
25413365

Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS

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