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5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit.
Mahy, William; Willis, Nicky J; Zhao, Yuguang; Woodward, Hannah L; Svensson, Fredrik; Sipthorp, James; Vecchia, Luca; Ruza, Reinis R; Hillier, James; Kjær, Svend; Frew, Sarah; Monaghan, Amy; Bictash, Magda; Salinas, Patricia C; Whiting, Paul; Vincent, Jean-Paul; Jones, E Yvonne; Fish, Paul V.
Afiliação
  • Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Zhao Y; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Sipthorp J; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Vecchia L; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Ruza RR; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Hillier J; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Kjær S; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Frew S; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.
  • Monaghan A; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
  • Bictash M; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Salinas PC; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Whiting P; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Vincent JP; Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K.
  • Jones EY; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.
  • Fish PV; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.
J Med Chem ; 63(21): 12942-12956, 2020 11 12.
Article em En | MEDLINE | ID: mdl-33124429
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Oxidiazóis / Inibidores Enzimáticos / Esterases Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Reino Unido
Texto completo
Adicionar na Minha BVS
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Oxidiazóis / Inibidores Enzimáticos / Esterases Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Animals / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Reino Unido