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المؤلفون: Patricia F Medeiros, Mythily Vimal, Vipulkumar Kantibhai Patel, John Evans, Neil R Carlson, Antonia J. Lewis, Paul Bamborough, Katherine L Jones, Jane E Smith, Michael O'Sullivan, Scott McCleary, Darren J. Mitchell, Heather Barnett, Chun-wa Chung, Gang Yao, Anthony W. J. Cooper, Rab K. Prinjha, Laurie Gordon, Mahnoor Mahmood, Peter D. Craggs, Isobel L Harada, Rino A Bit, Natalie Wellaway, Armelle Le Gall, Robert J. Watson, Tony W Dean, Dominique Amans, Ian D. Wall, Kayleigh A J Stafford, Dave Lugo, Matthew J Lindon, Rishi R Shah, David Jonathan Hirst, Chris Patten, Darren L Poole, Jack A Brown, Philip G Humphreys, Robert P Davis, Christopher Roland Wellaway, Pamela J Thomas
المصدر: Journal of Medicinal Chemistry. 63:714-746
مصطلحات موضوعية: Male, Models, Molecular, Benzimidazole, Lysine, Drug Evaluation, Preclinical, Computational biology, Crystallography, X-Ray, Small Molecule Libraries, Mice, chemistry.chemical_compound, In vivo, Histone tails, Drug Discovery, Leukocytes, Animals, Humans, Chemokine CCL2, Therapeutic strategy, Interleukin-6, Chemistry, Anti-Inflammatory Agents, Non-Steroidal, Proteins, Drug Synergism, Epigenome, Small molecule, High-Throughput Screening Assays, Bromodomain, Molecular Medicine, Benzimidazoles, Protein Processing, Post-Translational
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المؤلفون: Laurie J. Gordon, Matthew J Lindon, Nicholas C. O. Tomkinson, Chun-wa Chung, Isabelle Becher, Judit Molnar, Ka Hing Che, Paola Grandi, Andrew J. Bannister, David H. Drewry, Rab K. Prinjha, Antje Dittmann, Tony Kouzarides, Natalie Hope Theodoulou, Rino A. Bit, Philip G. Humphreys, Anne-Marie Michon, Samuel Robson, Gerard Drewes, Melanie Leveridge, Paul Bamborough
المصدر: 'Journal of Medicinal Chemistry ', vol: 59, pages: 1425-1439 (2016)
Theodoulou, N H, Bamborough, P, Bannister, A J, Becher, I, Bit, R A, Che, K H, Chung, C, Dittmann, A, Drewes, G, Drewry, D H, Gordon, L, Grandi, P, Leveridge, M, Lindon, M, Michon, A-M, Molnar, J, Robson, S C, Tomkinson, N C O, Kouzarides, T, Prinjha, R K & Humphreys, P G 2016, ' Discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition ', Journal of Medicinal Chemistry, vol. 59, no. 4, pp. 1425-1439 . https://doi.org/10.1021/acs.jmedchem.5b00256
J Med Chemمصطلحات موضوعية: Models, Molecular, 0301 basic medicine, Lysine, Crystallography, X-Ray, Article, Cell Line, Small Molecule Libraries, 03 medical and health sciences, Protein acylation, Transcription (biology), Drug Discovery, Humans, Amino Acid Sequence, Gene, Binding Sites, biology, Chemistry, Biomedical Sciences, Molecular biology, Bromodomain, Chromatin, Cell biology, Molecular Docking Simulation, QD450, 030104 developmental biology, Histone, Acetylation, biology.protein, Molecular Medicine, Transcription Factors
وصف الملف: application/pdf
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المؤلفون: Aarti Patel, Nigel Deeks, Maxine A. Taylor, Jason Witherington, Dung Nguyen, Robert J. Watson, Rino A. Bit, Fiona McClure, Emmanuel Hubert Demont, James Gray, Holly Ashall, Steve R. Hood, Simon Taylor
المصدر: Journal of Medicinal Chemistry. 58:8236-8256
مصطلحات موضوعية: Models, Molecular, Context (language use), Pharmacology, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, Dogs, Downregulation and upregulation, Cytochrome P-450 CYP1A2, In vivo, Drug Discovery, Cytochrome P-450 CYP1A1, Animals, Humans, RNA, Messenger, Receptor, biology, Drug discovery, Chemistry, Cytochrome P450, Lipids, In vitro, Rats, Up-Regulation, Macaca fascicularis, Receptors, Lysosphingolipid, Receptors, Aryl Hydrocarbon, Drug development, Drug Design, Enzyme Induction, Hepatocytes, biology.protein, Molecular Medicine
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المؤلفون: Robert J. Watson, David Norton, John Skidmore, Christopher N. Johnson, Gerard Martin Paul Giblin, Jennifer Sweeting, Rivers Dean Andrew, Mahmood Ahmed, Andrea C. Haynes, Ian D. Wall, Sally Redshaw, Karen Louise Philpott, Jason Witherington, David N. Hurst, Umesh Kumar, James Myatt, Simon Taylor, Emmanuel Hubert Demont, Alexander J. Stevens, Tom D. Heightman, Rino A. Bit, D. Vesey, Jag Paul Heer, Andrew Peter Cridland
المصدر: Journal of Medicinal Chemistry. 57:10424-10442
مصطلحات موضوعية: Male, Models, Molecular, Metabolite, Carboxylic Acids, Pharmacology, Structure-Activity Relationship, chemistry.chemical_compound, Pharmacokinetics, Heterocyclic Compounds, In vivo, Drug Discovery, medicine, Animals, Structure–activity relationship, Lymphocytes, Sphingosine-1-phosphate, Receptor, Cells, Cultured, Molecular Structure, Chemistry, Fingolimod, In vitro, Receptors, Lysosphingolipid, Biochemistry, Rats, Inbred Lew, Molecular Medicine, Immunosuppressive Agents, medicine.drug
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المؤلفون: Nigel Deeks, Robert J. Watson, James Matthew Bailey, Simon Taylor, Jessica F. Renaux, Andrea C. Haynes, Simon J. Dowell, Rino A. Bit, Colin David Eldred, Colin A. Campbell, Duncan S. Holmes, Jason Witherington, Umesh Kumar, Jack A. Brown, Mary A. Morse, Emmanuel Hubert Demont, Pam Gaskin, Chris A. Smethurst, Gail A. Seal, Greg J. Osborne, James Gray, Robert Willis, David Jonathan Hirst
المصدر: Journal of medicinal chemistry. 59(3)
مصطلحات موضوعية: 0301 basic medicine, Agonist, Drug, Male, medicine.drug_class, Pyridines, media_common.quotation_subject, Administration, Oral, Mice, Inbred Strains, Pharmacology, 01 natural sciences, Cell Line, Rats, Sprague-Dawley, 03 medical and health sciences, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Dogs, Drug Discovery, medicine, Structure–activity relationship, Animals, Humans, Receptor, Sphingosine-1-Phosphate Receptors, media_common, Sphingosine 1-Phosphate Receptor 3, Dose-Response Relationship, Drug, Molecular Structure, Drug discovery, Chemistry, Tetrahydroisoquinoline, 0104 chemical sciences, Rats, 010404 medicinal & biomolecular chemistry, Receptors, Lysosphingolipid, 030104 developmental biology, Rats, Inbred Lew, THIQ, Molecular Medicine, Pyrazoles, medicine.drug
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المؤلفون: Karen Louise Philpott, Robert J. Watson, Jason Witherington, Greg J. Osborne, Terry Panchal, Simon Taylor, Nigel Deeks, Tom D. Heightman, James Gray, Umesh Kumar, Simon J. Dowell, Pam Gaskin, Lee Andrew Harrison, Robert Willis, Colin A. Campbell, Sandra Arpino, Sapna Desai, Rino A. Bit, Mary A. Morse, Emmanuel Hubert Demont, Andrea C. Haynes, Philip G. Humphreys, Duncan S. Holmes
المصدر: Journal of Medicinal Chemistry. 54:6724-6733
مصطلحات موضوعية: Agonist, medicine.drug_class, Chemistry, organic chemicals, Multiple sclerosis, Central nervous system, Pharmacology, medicine.disease, Fingolimod, Therapeutic index, medicine.anatomical_structure, In vivo, Drug Discovery, medicine, Molecular Medicine, Potency, lipids (amino acids, peptides, and proteins), Receptor, medicine.drug
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المؤلفون: Andrea C. Haynes, Benjamin I. Andrews, Bela Rajiv Patel, Jason Witherington, Mary A. Morse, Umesh Kumar, Colin A. Campbell, Pam Gaskin, Sapna Desai, Robert Willis, Jason W. B. Cooke, Greg J. Osborne, Simon Taylor, Robert J. Watson, Terry Panchal, Alcide Perboni, Nigel Deeks, James Gray, Simon J. Dowell, Duncan S. Holmes, Rino A. Bit, Emmanuel Hubert Demont
المصدر: ACS Medicinal Chemistry Letters. 2:444-449
مصطلحات موضوعية: Agonist, Bradycardia, medicine.medical_specialty, Sphingosine, medicine.drug_class, business.industry, Multiple sclerosis, Organic Chemistry, Arthritis, Pharmacology, medicine.disease, Biochemistry, Fingolimod, chemistry.chemical_compound, Endocrinology, chemistry, Pharmacokinetics, Internal medicine, Drug Discovery, medicine, medicine.symptom, business, Receptor, medicine.drug
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المؤلفون: Mark Patrick Healy, Karamjit S. Jandu, Kim L. Matthews, James E. Rowedder, Clement Douault, Wenjing Meng, Andrew Billinton, Jason Witherington, Anne Hersey, Rino A. Bit, Nick M. Clayton, James Myatt, Gianpaolo Bravi, Christopher N. Johnson, Jason D. Brown, Livermore David
المصدر: Bioorganicmedicinal chemistry letters. 20(15)
مصطلحات موضوعية: Calcium Channels, L-Type, Stereochemistry, Pyridines, Clinical Biochemistry, Analgesic, Pharmaceutical Science, Ligands, Biochemistry, Structure-Activity Relationship, In vivo, Drug Discovery, Animals, ATP Binding Cassette Transporter, Subfamily B, Member 1, Molecular Biology, Analgesics, Chemistry, Ligand, Organic Chemistry, Calcium Channel Blockers, In vitro, Rats, Pyridazines, Neuropathic pain, Molecular Medicine, Neuralgia, Pyrazoles, Alpha-2 adrenergic receptor, Efflux, Calcium Channels, Selectivity
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المؤلفون: Adrian Hall, Gerard Martin Paul Giblin, David N. Hurst, Xiao Qing Lewell, Ian R. Kilford, Anita Chowdhury, Susan H. Brown, Alan Naylor, Rino A. Bit, Tiziana Scoccitti
المصدر: Bioorganicmedicinal chemistry letters. 18(5)
مصطلحات موضوعية: Models, Molecular, Molecular model, Isostere, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Pyrazole, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Structure-Activity Relationship, Heterocyclic Compounds, Drug Discovery, Pyridine, Receptors, Prostaglandin E, Methylene, skin and connective tissue diseases, Thiazole, Molecular Biology, Molecular Structure, fungi, Organic Chemistry, Receptors, Prostaglandin E, EP1 Subtype, body regions, chemistry, Molecular Medicine, Linker, Protein Binding
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المؤلفون: Stephen A. Hurst, Rino A. Bit, Davis Peter David
المصدر: Tetrahedron Letters. 31:2353-2356
مصطلحات موضوعية: chemistry.chemical_compound, Bicyclic molecule, chemistry, Intramolecular reaction, Acyl chloride, Organic Chemistry, Drug Discovery, Organic chemistry, Maleic anhydride, Condensation reaction, Biochemistry, Triethylamine