title: High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139.
abstract: OBJECTIVE
  To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules.
  
  
  METHODS
  Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies.
  
  
  RESULTS
  Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds.
  
  
  CONCLUSIONS
  The findings provide important tools for further study of this orphan G-protein coupled receptor.
authors.affiliation: The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Jia
authors.initials: J
authors.lastname: Wang
authors.affiliation: The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Lin-yun
authors.initials: LY
authors.lastname: Zhu
authors.affiliation: The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Liu
authors.affiliation: Neuroscience Drug Discovery, H Lundbeck A/S, DK-2500 Copenhagen, Denmark.
authors.forename: Morten
authors.initials: M
authors.lastname: Hentzer
authors.affiliation: Neuroscience Drug Discovery, H Lundbeck A/S, DK-2500 Copenhagen, Denmark.
authors.forename: Garrick Paul
authors.initials: GP
authors.lastname: Smith
authors.affiliation: The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Ming-wei
authors.initials: MW
authors.lastname: Wang
mesh_terms: D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: C501535:GPR139 protein, human; D009419:Nerve Tissue Proteins; D043562:Receptors, G-Protein-Coupled; D002118:Calcium