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المؤلفون: Wellaway CR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Baldwin IR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Bamborough P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Barker D; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Bartholomew MA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Dümpelfeld B; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, 69117 Heidelberg, Germany., Evans JP; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Fazakerley NJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Homes P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Keeling SP; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Lewell XQ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., McNab FW; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Morley J; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Needham D; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Neu M; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., van Oosterhout AJM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Pal A; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Reinhard FBM; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, 69117 Heidelberg, Germany., Rianjongdee F; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Robertson CM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Rowland P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Shah RR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Sherriff EB; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Sloan LA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Teague S; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Thomas DA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Wellaway N; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Wojno-Picon J; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Coe DM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2022 Jan 13; Vol. 65 (1), pp. 633-664. Date of Electronic Publication: 2021 Dec 20.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Aldehyde Oxidase/*metabolism , Janus Kinase Inhibitors/*pharmacokinetics , Lung/*metabolism, Administration, Intranasal ; Administration, Intravenous ; Animals ; Binding Sites ; Drug Delivery Systems ; Female ; Humans ; Janus Kinase Inhibitors/administration & dosage ; Janus Kinase Inhibitors/chemical synthesis ; Liver/metabolism ; Mice ; Mice, Inbred BALB C ; Models, Molecular ; Molecular Docking Simulation ; Quinazolines/chemical synthesis ; Quinazolines/pharmacokinetics ; Quinazolines/pharmacology ; Structure-Activity Relationship

المؤلفون: Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Gordon L, Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Gray JRJ, Harrison LA, Kruger RG; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Matteo JJ; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., McCabe MT; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Zhang XP; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Demont EH

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Aug 12; Vol. 64 (15), pp. 10772-10805. Date of Electronic Publication: 2021 Jul 13.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Furans/*pharmacology , Proteins/*antagonists & inhibitors , Pyrazoles/*pharmacology, Dose-Response Relationship, Drug ; Furans/chemistry ; Humans ; Molecular Structure ; Proteins/metabolism ; Pyrazoles/chemistry ; Structure-Activity Relationship

المؤلفون: Harrison LA; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Atkinson SJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bassil A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Gray JRJ; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Levernier E; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Lewis A; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Lugo D; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Messenger C; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Michon AM; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Mitchell DJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Preston A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Prinjha RK; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rioja I; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Seal JT; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Taylor S; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Wall ID; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Watson RJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Demont EH; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Aug 12; Vol. 64 (15), pp. 10742-10771. Date of Electronic Publication: 2021 Jul 07.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Cell Cycle Proteins/*antagonists & inhibitors , Pyridines/*pharmacology , Transcription Factors/*antagonists & inhibitors, Cell Cycle Proteins/metabolism ; Dose-Response Relationship, Drug ; Humans ; Models, Molecular ; Molecular Structure ; Pyridines/chemistry ; Structure-Activity Relationship ; Transcription Factors/metabolism

المؤلفون: Aylott HE; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Atkinson SJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bamborough P; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bassil A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Gordon L; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, Heidelberg 69117, Germany., Gray JRJ; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Harrison LA; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Hayhow TG; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Messenger C; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Mitchell D; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Phillipou A; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Preston A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Prinjha RK; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rianjongdee F; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rioja I; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Seal JT; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Wall ID; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Watson RJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Demont EH; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Mar 25; Vol. 64 (6), pp. 3249-3281. Date of Electronic Publication: 2021 Mar 04.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Cell Cycle Proteins/*antagonists & inhibitors , Protein Domains/*drug effects , Small Molecule Libraries/*chemistry , Small Molecule Libraries/*pharmacology , Transcription Factors/*antagonists & inhibitors, Cell Cycle Proteins/chemistry ; Cell Cycle Proteins/metabolism ; Drug Design ; Drug Discovery ; Humans ; Transcription Factors/chemistry ; Transcription Factors/metabolism

المؤلفون: Seal JT, Atkinson SJ, Aylott H, Bamborough P, Chung CW, Copley RCB, Gordon L, Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Gray JRJ, Harrison LA, Hayhow TG, Lindon M, Messenger C, Michon AM; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Mitchell D, Preston A, Prinjha RK, Rioja I, Taylor S; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Wall ID, Watson RJ, Woolven JM, Demont EH

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Sep 10; Vol. 63 (17), pp. 9093-9126. Date of Electronic Publication: 2020 Aug 30.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Ligands*, Anti-Inflammatory Agents/*chemistry , Transcription Factors/*antagonists & inhibitors, Administration, Oral ; Amides/chemistry ; Amides/metabolism ; Amides/pharmacokinetics ; Animals ; Anti-Inflammatory Agents/metabolism ; Anti-Inflammatory Agents/pharmacokinetics ; Binding Sites ; Cell Cycle Proteins/antagonists & inhibitors ; Cell Cycle Proteins/metabolism ; Crystallography, X-Ray ; Dogs ; Half-Life ; Humans ; Hydrogen Bonding ; Male ; Molecular Dynamics Simulation ; Protein Domains ; Rats ; Rats, Wistar ; Structure-Activity Relationship ; Transcription Factors/metabolism

المؤلفون: Wellaway CR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bamborough P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bernard SG; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Chung CW; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Craggs PD; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Cutler L; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Demont EH; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Evans JP; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Gordon L; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Karamshi B; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lewis AJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lindon MJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Mitchell DJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Rioja I; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Soden PE; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Taylor S; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Watson RJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Willis R; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Woolven JM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Wyspiańska BS; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Kerr WJ; Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Prinjha RK; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, United Kingdom.

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Sep 10; Vol. 63 (17), pp. 9020-9044. Date of Electronic Publication: 2020 Aug 03.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Drug Design*, Anti-Inflammatory Agents/*chemistry , Cell Cycle Proteins/*antagonists & inhibitors , Transcription Factors/*antagonists & inhibitors, Animals ; Anti-Inflammatory Agents/metabolism ; Anti-Inflammatory Agents/pharmacology ; Binding Sites ; Cell Cycle Proteins/classification ; Cell Cycle Proteins/metabolism ; Cell Line, Tumor ; Cytokines/metabolism ; Half-Life ; Humans ; Leukocytes, Mononuclear/cytology ; Leukocytes, Mononuclear/drug effects ; Leukocytes, Mononuclear/metabolism ; Male ; Mice ; Molecular Dynamics Simulation ; Phylogeny ; Protein Domains ; Quinolones/chemistry ; Quinolones/metabolism ; Quinolones/pharmacology ; Transcription Factors/classification ; Transcription Factors/metabolism

المؤلفون: Preston A; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Atkinson SJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Bamborough P; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Gordon LJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Grandi P; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Gray JRJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Harrison LA; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Lewis AJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Lugo D; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Messenger C; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Michon AM; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Mitchell DJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Prinjha RK; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Rioja I; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Seal J; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Taylor S; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Thesmar P; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Wall ID; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Watson RJ; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Demont EH; Epigenetics Discovery Performance Unit and Platform Technology and Science, GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Jul 06; Vol. 11 (8), pp. 1581-1587. Date of Electronic Publication: 2020 Jul 06 (Print Publication: 2020).

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101521073 Publication Model: eCollection Cited Medium: Print ISSN: 1948-5875 (Print) Linking ISSN: 19485875 NLM ISO Abbreviation: ACS Med Chem Lett Subsets: PubMed not MEDLINE

المؤلفون: Harris PA, Faucher N; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., George N; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Eidam PM, King BW, White GV; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Anderson NA; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Bandyopadhyay D, Beal AM, Beneton V; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Berger SB, Campobasso N, Campos S; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Capriotti CA, Cox JA, Daugan A; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Donche F; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Fouchet MH; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Finger JN, Geddes B, Gough PJ, Grondin P; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Hoffman BL, Hoffman SJ, Hutchinson SE; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Jeong JU, Jigorel E; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Lamoureux P; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Nagilla R, Nassau PM; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Ng SL, Ouellette MT, Pasikanti KK, Potvain F; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Reilly MA, Rivera EJ, Sautet S; Flexible Discovery Unit , GlaxoSmithKline , 25-27 avenue du Québec , 91951 Les Ulis Cedex , France., Schaeffer MC, Sehon CA, Sun H, Thorpe JH; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Totoritis RD, Ward P, Wellaway N; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Wisnoski DD, Woolven JM; Flexible Discovery Unit , GlaxoSmithKline , Gunnels Wood Road , Stevenage , Hertfordshire SG1 2NY , U.K., Bertin J, Marquis RW

المصدر: Journal of medicinal chemistry [J Med Chem] 2019 May 23; Vol. 62 (10), pp. 5096-5110. Date of Electronic Publication: 2019 May 02.

نوع المنشور: Journal Article

بيانات الدورية: 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

مواضيع طبية MeSH: Enzyme Inhibitors/*chemical synthesis , Enzyme Inhibitors/*pharmacology , Nuclear Pore Complex Proteins/*antagonists & inhibitors , Pyrazoles/*chemical synthesis , Pyrazoles/*pharmacology , RNA-Binding Proteins/*antagonists & inhibitors, Animals ; Biological Availability ; Cell Line ; Chronic Disease ; Drug Design ; Encephalomyelitis, Autoimmune, Experimental/drug therapy ; Enzyme Inhibitors/pharmacokinetics ; Haplorhini ; High-Throughput Screening Assays ; Humans ; Mice ; Mice, Inbred C57BL ; Models, Molecular ; Multiple Sclerosis/drug therapy ; Pyrazoles/pharmacokinetics ; Rats ; Retinitis Pigmentosa/drug therapy ; Structure-Activity Relationship