View in EDS

Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Saved in:
Bibliographic Details
Title: Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Authors: Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Gobbi A, Hawkins J; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Johnson AR, La H, Lesch J, Lockey P; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Norman M; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Ouyang W, Summerhill S; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Wong H
Source: Journal of medicinal chemistry [J Med Chem] 2015 Jul 09; Vol. 58 (13), pp. 5308-22. Date of Electronic Publication: 2015 Jun 23.
Publication Type: Journal Article; Research Support, N.I.H., Extramural
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
FullText Text:
  Availability: 0
Header DbId: mdl
DbLabel: MEDLINE Ultimate
An: 26061388
AccessLevel: 2
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
IllustrationInfo
Items – Name: Title
  Label: Title
  Group: Ti
  Data: Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
– Name: Author
  Label: Authors
  Group: Au
  Data: <searchLink fieldCode="AU" term="%22Fauber+BP%22">Fauber BP</searchLink><br /><searchLink fieldCode="AU" term="%22René+O%22">René O</searchLink><br /><searchLink fieldCode="AU" term="%22Deng+Y%22">Deng Y</searchLink><br /><searchLink fieldCode="AU" term="%22DeVoss+J%22">DeVoss J</searchLink><br /><searchLink fieldCode="AU" term="%22Eidenschenk+C%22">Eidenschenk C</searchLink><br /><searchLink fieldCode="AU" term="%22Everett+C%22">Everett C</searchLink><br /><searchLink fieldCode="AU" term="%22Ganguli+A%22">Ganguli A</searchLink>; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K.<br /><searchLink fieldCode="AU" term="%22Gobbi+A%22">Gobbi A</searchLink><br /><searchLink fieldCode="AU" term="%22Hawkins+J%22">Hawkins J</searchLink>; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K.<br /><searchLink fieldCode="AU" term="%22Johnson+AR%22">Johnson AR</searchLink><br /><searchLink fieldCode="AU" term="%22La+H%22">La H</searchLink><br /><searchLink fieldCode="AU" term="%22Lesch+J%22">Lesch J</searchLink><br /><searchLink fieldCode="AU" term="%22Lockey+P%22">Lockey P</searchLink>; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K.<br /><searchLink fieldCode="AU" term="%22Norman+M%22">Norman M</searchLink>; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K.<br /><searchLink fieldCode="AU" term="%22Ouyang+W%22">Ouyang W</searchLink><br /><searchLink fieldCode="AU" term="%22Summerhill+S%22">Summerhill S</searchLink>; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K.<br /><searchLink fieldCode="AU" term="%22Wong+H%22">Wong H</searchLink>
– Name: TitleSource
  Label: Source
  Group: Src
  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2015 Jul 09; Vol. 58 (13), pp. 5308-22. <i>Date of Electronic Publication: </i>2015 Jun 23.
– Name: TypePub
  Label: Publication Type
  Group: TypPub
  Data: Journal Article; Research Support, N.I.H., Extramural
– Name: TitleSource
  Label: Journal Info
  Group: Src
  Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE
PLink https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=26061388
RecordInfo BibRecord:
  BibEntity:
    Identifiers:
      – Type: doi
        Value: 10.1021/acs.jmedchem.5b00597
    Languages:
      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        StartPage: 5308
    Titles:
      – TitleFull: Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
        Type: main
  BibRelationships:
    HasContributorRelationships:
      – PersonEntity:
          Name:
            NameFull: Fauber BP
      – PersonEntity:
          Name:
            NameFull: René O
      – PersonEntity:
          Name:
            NameFull: Deng Y
      – PersonEntity:
          Name:
            NameFull: DeVoss J
      – PersonEntity:
          Name:
            NameFull: Eidenschenk C
      – PersonEntity:
          Name:
            NameFull: Everett C
      – PersonEntity:
          Name:
            NameFull: Ganguli A
      – PersonEntity:
          Name:
            NameFull: Gobbi A
      – PersonEntity:
          Name:
            NameFull: Hawkins J
      – PersonEntity:
          Name:
            NameFull: Johnson AR
      – PersonEntity:
          Name:
            NameFull: La H
      – PersonEntity:
          Name:
            NameFull: Lesch J
      – PersonEntity:
          Name:
            NameFull: Lockey P
      – PersonEntity:
          Name:
            NameFull: Norman M
      – PersonEntity:
          Name:
            NameFull: Ouyang W
      – PersonEntity:
          Name:
            NameFull: Summerhill S
      – PersonEntity:
          Name:
            NameFull: Wong H
    IsPartOfRelationships:
      – BibEntity:
          Dates:
            – D: 09
              M: 07
              Text: 2015 Jul 09
              Type: published
              Y: 2015
          Identifiers:
            – Type: issn-electronic
              Value: 1520-4804
          Numbering:
            – Type: volume
              Value: 58
            – Type: issue
              Value: 13
          Titles:
            – TitleFull: Journal of medicinal chemistry
              Type: main
ResultId 1