المؤلفون: Le Bihan, Y-V, Lanigan, RM, Atrash, B, McLaughlin, MG, Velupillai, S, Malcolm, AG, England, KS, Ruda, GF, Mok, NY, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, JM, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, FI, Fedorov, O, Brennan, PE, Burke, R, Van Montfort, RLM, Rossanese, OW, Blagg, J, Bavetsias, V

المصدر: European Journal of Medicinal Chemistry
Le Bihan, Y-V, Lanigan, R M, Atrash, B, McLaughlin, M G, Velupillai, S, Malcolm, A G, England, K S, Ruda, G F, Mok, N Y, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, J M, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, F I, Fedorov, O, Brennan, P, Burke, R, van Montfort, R L M, Rossanese, O W, Blagg, J & Bavetsias, V 2019, ' C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays ', European Journal of Medicinal Chemistry, vol. 177, pp. 316-337 . https://doi.org/10.1016/j.ejmech.2019.05.041

مصطلحات موضوعية: KDM4 subfamily, Jumonji Domain-Containing Histone Demethylases, Molecular Structure, Pyridines, Pyrimidinones, Crystallography, X-Ray, Article, Pyridopyrimidinones, Structure-Activity Relationship, Cell Line, Tumor, Humans, KDM inhibitors, Drug Screening Assays, Antitumor, Enzyme Inhibitors, KDM5 subfamily, Hydrophobic and Hydrophilic Interactions, Histone demethylases, Protein Binding

وصف الملف: application/pdf; text

URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::b23e38e79895cd396b4e21c1fb1c9678
http://europepmc.org/articles/PMC6580095

المؤلفون: Dolciami D; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K., Ziolek RM; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K., Davies DW; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K., Carter M; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K., Mok NY; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K., Sherhod R; BenevolentAI, 4-8 Maple Street, London W1T 5HD, U.K.

المصدر: Journal of chemical information and modeling [J Chem Inf Model] 2024 Mar 25; Vol. 64 (6), pp. 1966-1974. Date of Electronic Publication: 2024 Mar 04.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101230060 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1549-960X (Electronic) Linking ISSN: 15499596 NLM ISO Abbreviation: J Chem Inf Model Subsets: MEDLINE

مواضيع طبية MeSH: Cheminformatics* , Drug Discovery*, Humans ; Drug Design ; Molecular Structure ; Chemistry, Pharmaceutical

المؤلفون: Pasqua AE; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Sharp SY; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Chessum NEA; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Hayes A; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Pellegrino L; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Tucker MJ; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Miah A; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Wilding B; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Evans LE; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Rye CS; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Mok NY; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Liu M; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Henley AT; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Gowan S; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., De Billy E; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Te Poele R; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Powers M; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Eccles SA; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Clarke PA; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Raynaud FI; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Workman P; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Jones K; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom., Cheeseman MD; Centre for Cancer Drug Discovery and Division of Cancer Therapeutics at The Institute of Cancer Research, London SW7 3RP, United Kingdom.

المصدر: Journal of medicinal chemistry [J Med Chem] 2023 Apr 27; Vol. 66 (8), pp. 5907-5936. Date of Electronic Publication: 2023 Apr 05.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

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: Ovarian Neoplasms*/pathology , Antineoplastic Agents*/pharmacology, Humans ; Female ; Transcription Factors/metabolism ; Cell Line, Tumor

المؤلفون: Colombano G, Caldwell JJ, Matthews TP, Bhatia C; Department of Molecular and Cell Biology , University of Leicester , Leicester LE1 7RH , U.K., Joshi A; Department of Molecular and Cell Biology , University of Leicester , Leicester LE1 7RH , U.K., McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R; Department of Molecular and Cell Biology , University of Leicester , Leicester LE1 7RH , U.K.; School of Molecular and Cellular Biology, Faculty of Biological Sciences , University of Leeds , Leeds LS2 9JT , U.K., Collins I

المصدر: Journal of medicinal chemistry [J Med Chem] 2019 Mar 14; Vol. 62 (5), pp. 2447-2465. Date of Electronic Publication: 2019 Mar 05.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

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: Endoribonucleases/*antagonists & inhibitors , Endoribonucleases/*metabolism , Protein Kinase Inhibitors/*pharmacology , Protein Serine-Threonine Kinases/*antagonists & inhibitors , Protein Serine-Threonine Kinases/*metabolism, Allosteric Regulation ; Biopolymers/metabolism ; Crystallography, X-Ray ; Dimerization ; Endoplasmic Reticulum Stress/drug effects ; Endoribonucleases/chemistry ; HEK293 Cells ; Humans ; Phosphorylation ; Protein Conformation ; Protein Kinase Inhibitors/metabolism ; Protein Serine-Threonine Kinases/chemistry

المؤلفون: Meyers J; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Chessum NEA; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Ali S; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Mok NY; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Wilding B; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Pasqua AE; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Rowlands M; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Tucker MJ; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Evans LE; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Rye CS; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., O'Fee L; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Carter M; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Workman P; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Blagg J; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Brown N; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Jones K; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom., Cheeseman MD; Cancer Research UK Cancer Therapeutics Unit and Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, United Kingdom.

المصدر: ACS medicinal chemistry letters [ACS Med Chem Lett] 2018 Nov 16; Vol. 9 (12), pp. 1199-1204. Date of Electronic Publication: 2018 Nov 16 (Print Publication: 2018).

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: Hayes A; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Mok NY; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Liu M; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Thai C; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Henley AT; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Atrash B; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Lanigan RM; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Sejberg J; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Le Bihan YV; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Bavetsias V; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Blagg J; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Raynaud FI; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK.

المصدر: Xenobiotica; the fate of foreign compounds in biological systems [Xenobiotica] 2017 Sep; Vol. 47 (9), pp. 771-777. Date of Electronic Publication: 2016 Oct 26.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Informa Healthcare Country of Publication: England NLM ID: 1306665 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1366-5928 (Electronic) Linking ISSN: 00498254 NLM ISO Abbreviation: Xenobiotica Subsets: MEDLINE

مواضيع طبية MeSH: Aldehyde Oxidase/*antagonists & inhibitors , Pyrimidines/*metabolism, Animals ; Humans ; Mice ; Models, Molecular ; Proton Magnetic Resonance Spectroscopy ; Structure-Activity Relationship

المؤلفون: Mok NY; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , London, SM2 5NG, U.K., Brown N; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , London, SM2 5NG, U.K.

المصدر: Journal of chemical information and modeling [J Chem Inf Model] 2017 Jan 23; Vol. 57 (1), pp. 27-35. Date of Electronic Publication: 2016 Dec 19.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101230060 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1549-960X (Electronic) Linking ISSN: 15499596 NLM ISO Abbreviation: J Chem Inf Model Subsets: MEDLINE

مواضيع طبية MeSH: Drug Design*, Cyclooxygenase 2 Inhibitors/*chemistry , Cyclooxygenase 2 Inhibitors/*pharmacology, Drug Evaluation, Preclinical ; Structure-Activity Relationship

المؤلفون: Meyers J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, SM2 5NG, UK., Carter M; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, SM2 5NG, UK., Mok NY; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, SM2 5NG, UK., Brown N; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, SM2 5NG, UK.

المصدر: Future medicinal chemistry [Future Med Chem] 2016 Sep; Vol. 8 (14), pp. 1753-67. Date of Electronic Publication: 2016 Aug 30.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Future Science Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Drug Design*, Pharmaceutical Preparations/*chemistry , Small Molecule Libraries/*chemistry, Chemistry, Pharmaceutical ; Humans ; Molecular Structure ; Pharmaceutical Preparations/chemical synthesis ; Small Molecule Libraries/chemical synthesis

المؤلفون: Bavetsias V; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Lanigan RM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Ruda GF; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Atrash B; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., McLaughlin MG; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Tumber A; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Mok NY; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Dempster S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Boxall KJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Jeganathan F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Hatch SB; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Savitsky P; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Velupillai S; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Krojer T; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., England KS; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Sejberg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Thai C; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Donovan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Pal A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Scozzafava G; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Bennett JM; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Kawamura A; Chemistry Research Laboratory, University of Oxford , Mansfield Road, Oxford OX1 3TA, U.K., Johansson C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Botnar Research Centre, NIHR Oxford Biomedical Research Unit , Oxford OX3 7LD, U.K., Szykowska A; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Gileadi C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Burgess-Brown NA; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., von Delft F; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Diamond Light Source (DLS), Harwell Science and Innovation Campus , Didcot OX11 0DE, U.K.; Department of Biochemistry, University of Johannesburg , Auckland Park 2006, South Africa., Oppermann U; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Botnar Research Centre, NIHR Oxford Biomedical Research Unit , Oxford OX3 7LD, U.K., Walters Z; Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research , London SM2 5NG, U.K., Shipley J; Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research , London SM2 5NG, U.K., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Westaway SM; Epinova Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline R&D , Stevenage SG1 2NY, U.K., Prinjha RK; Epinova Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline R&D , Stevenage SG1 2NY, U.K., Fedorov O; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Schofield CJ; Chemistry Research Laboratory, University of Oxford , Mansfield Road, Oxford OX1 3TA, U.K., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Bountra C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Müller S; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Brennan PE; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Blagg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2016 Feb 25; Vol. 59 (4), pp. 1388-409. Date of Electronic Publication: 2016 Jan 07.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

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/*chemistry , Enzyme Inhibitors/*pharmacology , Jumonji Domain-Containing Histone Demethylases/*antagonists & inhibitors , Nuclear Proteins/*antagonists & inhibitors , Pyrimidinones/*chemistry , Pyrimidinones/*pharmacology , Repressor Proteins/*antagonists & inhibitors, Caco-2 Cells ; Cell Membrane Permeability ; Enzyme Inhibitors/pharmacokinetics ; Humans ; Jumonji Domain-Containing Histone Demethylases/chemistry ; Jumonji Domain-Containing Histone Demethylases/metabolism ; Nuclear Proteins/chemistry ; Nuclear Proteins/metabolism ; Pyrimidinones/pharmacokinetics ; Repressor Proteins/chemistry ; Repressor Proteins/metabolism

المؤلفون: Mok NY; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research , 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom., Brenk R, Brown N

المصدر: Journal of chemical information and modeling [J Chem Inf Model] 2014 Jan 27; Vol. 54 (1), pp. 79-85. Date of Electronic Publication: 2014 Jan 09.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101230060 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1549-960X (Electronic) Linking ISSN: 15499596 NLM ISO Abbreviation: J Chem Inf Model Subsets: MEDLINE

مواضيع طبية MeSH: Chemistry, Pharmaceutical/*methods , Drug Discovery/*methods , Drug Evaluation, Preclinical/*methods, Chemistry, Pharmaceutical/statistics & numerical data ; Computational Biology ; Databases, Chemical ; Databases, Pharmaceutical ; Drug Discovery/statistics & numerical data ; Drug Evaluation, Preclinical/statistics & numerical data ; Models, Cardiovascular ; Molecular Structure ; Principal Component Analysis