title: 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 S1P₁ agonists.
abstract: S1P(1) receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P(1) receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acid S1P(1) receptor agonists.
authors.affiliation: Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.
authors.forename: Daniel
authors.initials: D
authors.lastname: Buzard
authors.forename: Sangdon
authors.initials: S
authors.lastname: Han
authors.forename: Lars
authors.initials: L
authors.lastname: Thoresen
authors.forename: Jeanne
authors.initials: J
authors.lastname: Moody
authors.forename: Luis
authors.initials: L
authors.lastname: Lopez
authors.forename: Andrew
authors.initials: A
authors.lastname: Kawasaki
authors.forename: Thomas
authors.initials: T
authors.lastname: Schrader
authors.forename: Carleton
authors.initials: C
authors.lastname: Sage
authors.forename: Yinghong
authors.initials: Y
authors.lastname: Gao
authors.forename: Jeff
authors.initials: J
authors.lastname: Edwards
authors.forename: Jeremy
authors.initials: J
authors.lastname: Barden
authors.forename: Jayant
authors.initials: J
authors.lastname: Thatte
authors.forename: Lixia
authors.initials: L
authors.lastname: Fu
authors.forename: Michelle
authors.initials: M
authors.lastname: Solomon
authors.forename: Ling
authors.initials: L
authors.lastname: Liu
authors.forename: Hussien
authors.initials: H
authors.lastname: Al-Shamma
authors.forename: Joel
authors.initials: J
authors.lastname: Gatlin
authors.forename: Minh
authors.initials: M
authors.lastname: Le
authors.forename: Charles
authors.initials: C
authors.lastname: Xing
authors.forename: Sheryll
authors.initials: S
authors.lastname: Espinola
authors.forename: Robert M
authors.initials: RM
authors.lastname: Jones
mesh_terms: D000818:Animals; D001327:Autoimmune Diseases / Q000188:drug therapy*; D002087:Butyrates / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004195:Disease Models, Animal; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D000882:Haplorhini; D057166:High-Throughput Screening Assays; D006801:Humans; D007166:Immunosuppressive Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D008214:Lymphocytes / Q000378:metabolism*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009419:Nerve Tissue Proteins / Q000819:agonists* / Q000737:chemistry; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D016601:RNA-Binding Proteins / Q000819:agonists* / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D002087:Butyrates; C108381:GEMIN2 protein, human; D007166:Immunosuppressive Agents; D007211:Indoles; D009419:Nerve Tissue Proteins; D010069:Oxadiazoles; D016601:RNA-Binding Proteins