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1Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III
المؤلفون: Andrew Hebert, Paul Erdman, Maniar Sachin, Anlai Wang, Alexandre Gross, Elina Tserlin, Claude Barberis, Vinod F. Patel, Jiang John Z, Mark Czekaj, Mikhail Levit, James Pribish, Frank Sun, Matthieu Barrague, Luke Fire, Shih-Min A. Huang
المصدر: Bioorganicmedicinal chemistry letters. 29(3)
مصطلحات موضوعية: Indoles, Clinical Biochemistry, hERG, Compound 17, Pharmaceutical Science, Antineoplastic Agents, 01 natural sciences, Biochemistry, Part iii, Mice, Structure-Activity Relationship, Proto-Oncogene Proteins c-pim-1, Cell Line, Tumor, Drug Discovery, Animals, Humans, Molecular Biology, Protein Kinase Inhibitors, Cell Proliferation, biology, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Chemistry, Organic Chemistry, Neoplasms, Experimental, Combinatorial chemistry, 0104 chemical sciences, Rats, 010404 medicinal & biomolecular chemistry, Pim kinases, biology.protein, Molecular Medicine, Tumor growth inhibition, Drug Screening Assays, Antitumor
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2
المؤلفون: Sachin Maniar, Anlai Wang, James Pribish, Shih-Min A. Huang, Andrew Hebert, Mikhail Levit, Jinyu Liu, Claude Barberis, Luke Fire, Elina Tserlin, Paul Erdman, Vinod F. Patel, Mark Czekaj, Joseph D. Batchelor, Frank Sun
المصدر: Bioorganic & Medicinal Chemistry Letters. 30:127625
مصطلحات موضوعية: Indoles, Pyrrolidines, Clinical Biochemistry, hERG, Pharmaceutical Science, Antineoplastic Agents, Crystallography, X-Ray, 01 natural sciences, Biochemistry, Mice, Piperidines, Proto-Oncogene Proteins c-pim-1, Cell Line, Tumor, Drug Discovery, medicine, Animals, Humans, Tumor growth, Protein Kinase Inhibitors, Molecular Biology, PK/PD models, Aza Compounds, biology, 010405 organic chemistry, Chemistry, Kinase, Organic Chemistry, Cancer, Stereoisomerism, medicine.disease, Xenograft Model Antitumor Assays, Rats, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Permeability (electromagnetism), biology.protein, Cancer research, Molecular Medicine, Tumor growth inhibition, Protein Binding
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3
المؤلفون: James Pribish, Claude Barberis, Liduo Shen, Mark Czekaj, Neil Moorcroft, Mikhail Levit, Elina Tserlin, Anlai Wang, Andrew Hebert, Sandra Moreno-Mazza, Matthieu Barrague, Tahir Majid, Joseph D. Batchelor, Paul Erdman, Alexandre Gross
المصدر: Bioorganicmedicinal chemistry letters. 27(20)
مصطلحات موضوعية: 0301 basic medicine, Indoles, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Crystallography, X-Ray, Biochemistry, 03 medical and health sciences, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, 0302 clinical medicine, Proto-Oncogene Proteins c-pim-1, hemic and lymphatic diseases, Drug Discovery, Animals, Humans, Molecular Biology, Protein Kinase Inhibitors, PK/PD models, ADME, Kinase, Chemistry, Organic Chemistry, Hit to lead, Combinatorial chemistry, Rats, Enzyme Activation, 030104 developmental biology, 030220 oncology & carcinogenesis, Microsomes, Liver, Molecular Medicine, Identification (biology), Half-Life
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4
المؤلفون: Michael Gardyan, Mathew Rose M, Jane Davidson, Joseph Romano, Alain Dupuy, Aldous Suzanne C, Jennifer Kwong, Sam S. Rebello, Jennifer Cairns, Odessa Giardino, Yongyi Luo, Sébastien Maignan, Andrew David Morley, Clive Mccarthy, Joseph T. Tsay, Darren Engers, Guyan Liang, Houille Olivier, Julian Levell, Pribish James R, Jean-Pierre Guilloteau, Garry Fenton, Simon Watson, Trevor K.P. Harrison, Peter C. Astles, Liduo Shen, Mark Czekaj, Gregory H. Merriman, Keith Sides, Pauls Henry W, Keith Smith, Jie Wang, Heng-Keang Lim, Paul R. Eastwood, Brian Whiteley
المصدر: Bioorganic & Medicinal Chemistry. 13:2859-2872
مصطلحات موضوعية: Models, Molecular, Serine Proteinase Inhibitors, Arginine, Protein Conformation, Clinical Biochemistry, Administration, Oral, Biological Availability, Pharmaceutical Science, Tryptase, Crystallography, X-Ray, Biochemistry, Benzamidine, Structure-Activity Relationship, chemistry.chemical_compound, Piperidines, Drug Discovery, medicine, Animals, Humans, Molecular Biology, chemistry.chemical_classification, Serine protease, Molecular Structure, biology, Chemistry, Serine Endopeptidases, Organic Chemistry, Mast cell, Amides, Benzamidines, Recombinant Proteins, Rats, Enzyme, medicine.anatomical_structure, Liver, Enzyme inhibitor, Drug Design, biology.protein, Molecular Medicine, Tryptases, Caco-2 Cells, Factor Xa Inhibitors
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5
المؤلفون: Sebastian Maignan, Suzanne R Morgan, Robert J. Leadley, Valeria Chu, Gardner Charles J, Spada Alfred P, Pauls Henry W, Ross G. Bentley, Christopher T Dunwiddie, Klein Scott I, Jean-Pierre Guilloteau, Mark Czekaj, Karen Brown, Daniel L Cheney, Dennis J Colussi, Christopher L Heran, Kevin R. Guertin, Allison L Zulli, Yong Gong
المصدر: Bioorganic & Medicinal Chemistry Letters. 12:1671-1674
مصطلحات موضوعية: Models, Molecular, Serine Proteinase Inhibitors, medicine.drug_mechanism_of_action, Pyridines, Clinical Biochemistry, Factor Xa Inhibitor, Pharmaceutical Science, Crystallography, X-Ray, Biochemistry, Chemical synthesis, Cyclic N-Oxides, Amidine, chemistry.chemical_compound, In vivo, Drug Discovery, Hydrolase, medicine, Humans, Molecular Biology, chemistry.chemical_classification, Molecular Structure, biology, Organic Chemistry, Anticoagulants, Esters, In vitro, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Factor Xa Inhibitors
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6
المؤلفون: Mark Czekaj, Valeria Chu, Scott I. Klein, Bruce F. Molino
المصدر: European Journal of Medicinal Chemistry. 32:833-839
مصطلحات موضوعية: Pharmacology, chemistry.chemical_classification, Tetrapeptide, Fibrinogen receptor, Stereochemistry, medicine.drug_class, Organic Chemistry, Peptide, Carboxamide, General Medicine, Fibrinogen, Chemical synthesis, Combinatorial chemistry, chemistry, Drug Discovery, medicine, Platelet aggregation inhibitor, Platelet, medicine.drug
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7
المؤلفون: Robert J. Leadley, Bruce F. Molino, Scott I. Klein, Jeffrey S Dener, Christopher T. Dunwiddie, Ralph D. Sabatino, Mark Czekaj, Valeria Chu
المصدر: Bioorganic & Medicinal Chemistry Letters. 6:1403-1408
مصطلحات موضوعية: chemistry.chemical_classification, Scaffold, Stereochemistry, Fibrinogen receptor, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Peptide, Biochemistry, Non peptide, Combinatorial chemistry, chemistry.chemical_compound, chemistry, Drug Discovery, Molecular Medicine, Piperidine, Molecular Biology
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8
المؤلفون: Henry W. Pauls, Yong Gong, Mark Czekaj, Valeria Chu, Jingbo Gao, Karen D. Brown, Dennis J. Colussi, Alfred P. Spada, Guyan Liang
المصدر: ChemInform. 31
مصطلحات موضوعية: Serine, Proteases, Stereochemistry, Chemistry, Coagulation Factor Xa, General Medicine
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9
المؤلفون: Daniel L Cheney, Pauls Henry W, Christopher T Dunwiddie, Gardner Charles J, Kevin R. Guertin, Spada Alfred P, Allison L Zulli, Robert J. Leadley, Klein Scott I, Karen Brown, Valeria Chu, Dennis J Colussi, Mark Czekaj
المصدر: Bioorganicmedicinal chemistry letters. 12(12)
مصطلحات موضوعية: Proteases, Serine Proteinase Inhibitors, medicine.drug_mechanism_of_action, Clinical Biochemistry, Factor Xa Inhibitor, Pharmaceutical Science, Biochemistry, Amidine, chemistry.chemical_compound, Drug Discovery, medicine, Potency, Molecular Biology, chemistry.chemical_classification, biology, Organic Chemistry, Esters, In vitro, Enzyme, chemistry, Coagulation, Enzyme inhibitor, biology.protein, Molecular Medicine, Factor Xa Inhibitors
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10
المؤلفون: Mark Czekaj, Valeria Chu, Karen D. Brown, Scott I. Klein, Dennis J. Colussi, Robert J. Leadley, Christopher Heran, Ross Bentley, Charles Kasiewski, Mark H. Perrone, Suzanne Morgan, Jeffrey S. Bostwick
المصدر: European journal of pharmacology. 389(2-3)
مصطلحات موضوعية: Male, Bleeding Time, medicine.drug_mechanism_of_action, Factor Xa Inhibitor, Amidines, Pharmacology, Arginine, Argatroban, Rats, Sprague-Dawley, chemistry.chemical_compound, Fibrinolytic Agents, Antithrombotic, medicine, Animals, Platelet activation, Carotid Artery Thrombosis, Thrombus, Sulfonamides, medicine.diagnostic_test, Dose-Response Relationship, Drug, business.industry, Heparin, Factor X, medicine.disease, Rats, chemistry, Anesthesia, Pipecolic Acids, Benzamides, Partial Thromboplastin Time, business, medicine.drug, Partial thromboplastin time, Factor Xa Inhibitors