-
1
المؤلفون: Peng Gao, Paolo Vincetti, Fabio Maria Sabbatini, Holly J. Carlisle, Luisa Mengatto, Stéphane De Lombaert, Anna Sava, Kerry Zobel, Xinying Liu, Claudia Beato, Jessica M. Bright, Alyssa M. A. Toda, Elena Serra, Federica Budassi, Marco Migliore, Laura Caberlotto, Cristiana Griffante, Silvia Bernardi, Mingliang Zhang, Albert W. Garofalo, Daniele Andreotti
المصدر: Journal of Medicinal Chemistry. 63:14821-14839
مصطلحات موضوعية: Indazoles, Tetrazoles, Leucine-Rich Repeat Serine-Threonine Protein Kinase-2, 01 natural sciences, Small Molecule Libraries, Mice, Structure-Activity Relationship, 03 medical and health sciences, Drug Discovery, Animals, Humans, Kinase activity, Protein Kinase Inhibitors, Gene, 030304 developmental biology, 0303 health sciences, Molecular Structure, Chemistry, Kinase, Highly selective, LRRK2, High-Throughput Screening Assays, nervous system diseases, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, HEK293 Cells, Pyrimidines, Mutation, Cancer research, Molecular Medicine
-
2
المؤلفون: Qing Zhang, William J. Zavadoski, Robert J. Aiello, M.C. Holt, Nicole Barucci, Jim Valentine, A.J. Stein, Vishwas M. Paralkar, Stéphane De Lombaert, Daniel R. Goldberg, Patricia Bourassa
المصدر: Bioorganic & Medicinal Chemistry Letters. 27:413-419
مصطلحات موضوعية: 0301 basic medicine, Serotonin, Proline, Clinical Biochemistry, Pharmaceutical Science, Tryptophan Hydroxylase, Pharmacology, Biochemistry, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, 03 medical and health sciences, Dogs, 0302 clinical medicine, Oral administration, In vivo, Drug Discovery, Animals, Humans, Prodrugs, Spiro Compounds, Intestinal Mucosa, Molecular Biology, Binding Sites, TPH1, Chemistry, Organic Chemistry, Prodrug, Tryptophan hydroxylase, Oxidoreductase inhibitor, Protein Structure, Tertiary, Rats, Intestines, Molecular Docking Simulation, Pyrimidines, 030104 developmental biology, 030220 oncology & carcinogenesis, Molecular Medicine, Half-Life
-
3
المؤلفون: Nicole Barucci, Stéphane De Lombaert, Vishwas M. Paralkar, Jim Valentine, William J. Zavadoski, Patricia Bourassa, Robert J. Aiello, A.J. Stein, Daniel R. Goldberg, Qing Zhang
المصدر: Bioorganic & Medicinal Chemistry Letters. 26:2855-2860
مصطلحات موضوعية: Models, Molecular, 0301 basic medicine, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Tryptophan Hydroxylase, Biochemistry, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Biosynthesis, Drug Discovery, Humans, Structure–activity relationship, Enzyme Inhibitors, Guanidine, Molecular Biology, 5-HT receptor, TPH1, Dose-Response Relationship, Drug, Molecular Structure, Organic Chemistry, Tryptophan hydroxylase, Oxidoreductase inhibitor, 030104 developmental biology, chemistry, 030220 oncology & carcinogenesis, Molecular Medicine, Serotonin
-
4
المؤلفون: Patricia Bourassa, Nicole Barucci, Stéphane De Lombaert, William J. Zavadoski, Daniel R. Goldberg, Qing Zhang, Robert J. Aiello, James J. Valentine, Vishwas M. Paralkar
المصدر: Bioorganic & Medicinal Chemistry Letters. 26:1124-1129
مصطلحات موضوعية: 0301 basic medicine, Serotonin, Proline, Clinical Biochemistry, Pharmaceutical Science, Tryptophan Hydroxylase, Inhibitory postsynaptic potential, Biochemistry, Inhibitory Concentration 50, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Drug Discovery, Animals, Humans, Spiro Compounds, Neurotransmitter, Molecular Biology, chemistry.chemical_classification, Binding Sites, TPH1, Aryl, Organic Chemistry, Brain, Protein Structure, Tertiary, Rats, Amino acid, Molecular Docking Simulation, 030104 developmental biology, Monoamine neurotransmitter, chemistry, Drug Design, Molecular Medicine, Half-Life, Protein Binding
-
5
المؤلفون: Adam Flegg, Tina Morwick, Ho Yin Lo, Todd Bosanac, Weimin Liu, Valentina Berger, Steven Kerr, Stéphane De Lombaert, Paige Erin Mahaney, Ralph Binetti, John Broadwater, Spencer Napier, Alessandra Bartolozzi, Lifen Wu, Hidenori Takahashi, Asitha Abeywardane, Heather Tye, Tazmeen Fadra-Khan, John D. Huber, Adrian Kotey, Ming-Hong Hao, Dines Jonathon Alan, Anil Kumar Padyana, Alan Olague, Michael Garrigou, David S. Thomson, J. Matthew Hutzler, Pui Leng Loke, Renee Zindell, Edward Pack, Zhidong Chen, Rebecca Crux, Thomas Simpson, Rajvee Dave, Doris Riether
المصدر: Journal of Medicinal Chemistry. 58:1669-1690
مصطلحات موضوعية: Models, Molecular, Oxadiazoles, Arachidonate 5-Lipoxygenase, Dose-Response Relationship, Drug, CYP3A4, Stereochemistry, Chemistry, Molecular Conformation, Oxadiazole, 5-Lipoxygenase-Activating Protein Inhibitors, Crystallography, X-Ray, Structure-Activity Relationship, chemistry.chemical_compound, Pharmacokinetics, Acetamides, Drug Discovery, Humans, Molecular Medicine, Lipoxygenase Inhibitors, IC50, Ex vivo, Drug metabolism, Whole blood
-
6
المؤلفون: Xiang Li, Hidenori Takahashi, Steven S. Pullen, Stéphane De Lombaert, Asitha Abeywardane, Ming-Hong Hao, John R. Proudfoot, Anil Kumar Padyana, Brandon Collins, Leslie Martin, Daniel R. Albaugh, Steven John Taylor, Shuang Liang, Bennett Sandy Farmer, Melissa Hill-Drzewi
المصدر: Journal of Medicinal Chemistry. 56:4465-4481
مصطلحات موضوعية: Models, Molecular, Serine Proteinase Inhibitors, Molecular Structure, Chymase, Cardiovascular Agents, In Vitro Techniques, Cathepsin G, Crystallography, X-Ray, Structure-Activity Relationship, chemistry.chemical_compound, Chymases, chemistry, Biochemistry, Fragment (logic), Catalytic Domain, Drug Discovery, Microsomes, Liver, Screening method, Humans, Molecular Medicine, Benzimidazoles, Oxindole, Protein Binding
-
7
المؤلفون: Jeffrey Dubins, Marc Humbert, Christophe Guignabert, Vishwas Paralkar, Stéphane De Lombaert, Qing Zhang, Maria A. Cavasin, Robert J. Aiello, Timothy A. McKinsey, Daniel R. Goldberg, Patricia-Ann Bourassa
المصدر: The Journal of pharmacology and experimental therapeutics. 360(2)
مصطلحات موضوعية: 0301 basic medicine, Male, medicine.medical_specialty, Serotonin, Ambrisentan, Hypertension, Pulmonary, Myocytes, Smooth Muscle, Vasodilation, 030204 cardiovascular system & hematology, Biology, Pulmonary Artery, Tryptophan Hydroxylase, Vascular Remodeling, Gene Expression Regulation, Enzymologic, Rats, Sprague-Dawley, 03 medical and health sciences, 0302 clinical medicine, Internal medicine, medicine, Animals, Humans, Enzyme Inhibitors, Lung, Semaxanib, Cell Proliferation, Pharmacology, TPH1, Mast cell, medicine.disease, Pulmonary hypertension, Tadalafil, Rats, Disease Models, Animal, 030104 developmental biology, medicine.anatomical_structure, Endocrinology, HEK293 Cells, Molecular Medicine, medicine.drug
-
8
المؤلفون: Raymond A. Kemper, Jennifer Burke, James V. Haist, Nelamangara Nagaraja, Charles A. Kennedy, Christian Eickmeier, Stephen J. Boyer, Stéphane De Lombaert, Xin Guo, John D. Huber, Alan David Swinamer, Jeffrey B. Madwed, Anne B. Eldrup, Kirrane Thomas M, Morris Karmazyn, Fariba Soleymanzadeh, Paul Kaplita, Eugene R. Hickey, Jörg Bentzien, Elizabeth Mainolfi
المصدر: Journal of Medicinal Chemistry. 55:7114-7140
مصطلحات موضوعية: Blood Platelets, Male, Models, Molecular, ERG1 Potassium Channel, Cell Membrane Permeability, Sodium-Hydrogen Exchangers, Intracellular pH, Myocardial Infarction, Ischemia, Biological Availability, Myocardial Reperfusion Injury, Pharmacology, Guanidines, Permeability, Calcium in biology, Cell Line, Rats, Sprague-Dawley, Structure-Activity Relationship, Dogs, Drug Discovery, medicine, Animals, Cytochrome P-450 Enzyme Inhibitors, Humans, Protein Isoforms, Cell damage, Cell Size, Myocardial stunning, Sodium-Hydrogen Exchanger 1, Chemistry, Membranes, Artificial, medicine.disease, Ether-A-Go-Go Potassium Channels, Rats, Sodium–hydrogen antiporter, Benzamides, Microsomes, Liver, Molecular Medicine, Reperfusion injury, Ex vivo
-
9
المؤلفون: Ming-Hong Hao, E. Michael August, Danielle M. Fowler, Jin Mi Kim, Neil A. Farrow, Stéphane De Lombaert, Peter Allen Nemoto, Hidenori Takahashi, Leslie Martin, Daniel R. Albaugh, Steven S. Pullen, Kevin Chungeng Qian, Ho Yin Lo, Melissa Hill-Drzewi, Richard D. Schneiderman
المصدر: Bioorganic & Medicinal Chemistry Letters. 21:4533-4539
مصطلحات موضوعية: Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Crystallography, X-Ray, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Chymases, Drug Discovery, Side chain, Humans, Moiety, Protease Inhibitors, Molecular Biology, Indole test, Binding Sites, Organic Chemistry, Chymase, Benzothiophene, Glutathione, Protein Structure, Tertiary, chemistry, Molecular Medicine, Benzimidazoles, Hydrophobic and Hydrophilic Interactions, Oxidation-Reduction, Lead compound, Conjugate
-
10
المؤلفون: Stéphane De Lombaert, Diane M. Hargrove, Christine M. Mack, Charles A. Blum, David A. Griffith, Martin Sanders, Colin R. Rose, Tristan S. Maurer, John Inthavongsay, Lee E. Klade, Philip A. Carpino
المصدر: Bioorganic & Medicinal Chemistry Letters. 21:2641-2645
مصطلحات موضوعية: Pyrimidine, Pyridines, Clinical Biochemistry, Pharmaceutical Science, Neuropeptide, Blood Pressure, Pharmacology, Biochemistry, Rats, Sprague-Dawley, Eating, Mice, chemistry.chemical_compound, Oral administration, In vivo, Appetite Depressants, Drug Discovery, Animals, Humans, Pyrazolones, Receptor, Molecular Biology, Molecular Structure, Chemistry, Organic Chemistry, Antagonist, Rats, Receptors, Neuropeptide Y, Pyrimidines, Anorectic, Pyrazoles, Molecular Medicine, Efflux
-
11
المؤلفون: Alison Kukulka, Ho Yin Lo, Roman Wolfgang Fleck, Raj Betageri, Mary Ann Hoermann, Usha R. Patel, Stéphane De Lombaert, Alisa K. Kabcenell, Richard H. Ingraham, Rajiv Sharma, Kirrane Thomas M, John R. Proudfoot, Neil A. Farrow, Chuk Chui Man
المصدر: Bioorganic & Medicinal Chemistry Letters. 20:6379-6383
مصطلحات موضوعية: Models, Molecular, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Pyrazole, Crystallography, X-Ray, Biochemistry, Catalysis, Pyridazine, chemistry.chemical_compound, Aniline, Catalytic Domain, Drug Discovery, Hydrolase, Cytochrome P-450 CYP3A, Humans, Enzyme Inhibitors, Molecular Biology, Epoxide Hydrolases, CYP3A4, Chemistry, Organic Chemistry, Antagonist, Microsomes, Liver, cardiovascular system, Microsome, Cytochrome P-450 CYP3A Inhibitors, Pyrazoles, Molecular Medicine, Caco-2 Cells
-
12
المؤلفون: Harry Brielmann, David J. Matson, Bertrand L. Chenard, Mark T. Kershaw, W. Rycroft, Nicola Burnaby-Davies, Marci Crandall, Stéphane De Lombaert, Kevin J. Hodgetts, William J. Martin, Rajagopal Bakthavatchalam, Beth Ann Murphy, Timothy M. Caldwell, G Mason, A. Brian Jones, Xiaozhang Zheng, Helen Perrett, Susan Boyce, James E. Krause, Daniel N. Cortright, Charles A. Blum, Rachael Conley, Scott M. Capitosti
المصدر: Journal of Medicinal Chemistry. 53:3330-3348
مصطلحات موضوعية: Hot Temperature, Pyridines, TRPV1, Biological Availability, Pain, TRPV Cation Channels, In Vitro Techniques, Pharmacology, Structure-Activity Relationship, Transient receptor potential channel, chemistry.chemical_compound, Oral administration, In vivo, Chlorocebus aethiops, Drug Discovery, Noxious stimulus, Animals, Humans, Naphthyridines, Inflammation, Analgesics, Antagonist, Rats, Pyrimidines, chemistry, Discovery and development of TRPV1 antagonists, Hyperalgesia, Capsaicin, Pyrazines, COS Cells, Microsomes, Liver, Quinazolines, Quinolines, Molecular Medicine
-
13
المؤلفون: Stéphane De Lombaert, Ingo Muegge, Anne Bettina Eldrup, Neil A. Farrow, David Joseph, Keith McKellop, Fariba Soleymanzadeh, Chuk Chui Man, Steven John Taylor, Alison Kukulka
المصدر: Journal of Medicinal Chemistry. 52:5880-5895
مصطلحات موضوعية: Niacinamide, Epoxide hydrolase 2, Metabolite, Drug Evaluation, Preclinical, Administration, Oral, chemistry.chemical_compound, In vivo, Drug Discovery, Hydrolase, Animals, Humans, Enzyme Inhibitors, Epoxide Hydrolases, chemistry.chemical_classification, Molecular Structure, Metabolism, Rats, Enzyme, Solubility, chemistry, Biochemistry, Microsomes, Liver, Microsome, Molecular Medicine, Half-Life
-
14
المؤلفون: Jayaraman Chandrasekhar, Raymond F. Horvath, Ping Ge, Stéphane De Lombaert, Hutchison Alan J, Kevin J. Hodgetts, Dario Doller, Robbin Brodbeck, James E. Krause, Diane Hoffman, Michael Gulianello, Yoon Taeyoung, John H. Kehne
المصدر: Bioorganic & Medicinal Chemistry Letters. 18:4486-4490
مصطلحات موضوعية: Pyrimidine, Stereochemistry, Chemistry, Pharmaceutical, Clinical Biochemistry, Molecular Conformation, Pharmaceutical Science, Ether, Receptors, Corticotropin-Releasing Hormone, Biochemistry, Chemical synthesis, Rats, Sprague-Dawley, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Drug Discovery, Animals, Humans, Receptor, Molecular Biology, Binding Sites, Molecular Structure, Organic Chemistry, Antagonist, In vitro, Rats, Kinetics, Pyrimidines, Models, Chemical, Solubility, chemistry, Drug Design, Lipophilicity, Molecular Medicine
-
15
المؤلفون: Rajagopal Bakthavatchalam, Lawrence K. Fung, Bertrand L. Chenard, David J. Matson, Chu K. Ngo, Marci Crandall, Stéphane De Lombaert, Daniel N. Cortright, Harry Brielmann, Charles A. Blum, Mark T. Kershaw, Jayaraman Chandrasekhar, Marta Day, Xiaozhang Zheng, James E. Krause, Kevin J. Hodgetts
المصدر: Bioorganic & Medicinal Chemistry Letters. 18:4573-4577
مصطلحات موضوعية: Drug, ERG1 Potassium Channel, Stereochemistry, Chemistry, Pharmaceutical, media_common.quotation_subject, Clinical Biochemistry, Analgesic, Molecular Conformation, TRPV1, Pain, TRPV Cation Channels, Pharmaceutical Science, Pharmacology, Biochemistry, Dogs, Oral administration, In vivo, Drug Discovery, medicine, Animals, Potency, Molecular Biology, media_common, Inflammation, Chemistry, Organic Chemistry, Antagonist, Ether-A-Go-Go Potassium Channels, Rats, Kinetics, Models, Chemical, Pharmaceutical Preparations, Drug Design, Hyperalgesia, Aminoquinolines, Molecular Medicine, medicine.symptom
-
16
المؤلفون: Diane Hoffman, Ping Ge, Raymond F. Horvath, Kevin J. Hodgetts, Yoon Taeyoung, John H. Kehne, Stéphane De Lombaert, James E. Krause, Michael Gulianello, Mark T. Kershaw, Jayaraman Chandrasekhar, Robbin Brodbeck, Dario Doller
المصدر: Bioorganic & Medicinal Chemistry Letters. 18:891-896
مصطلحات موضوعية: medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Anxiety, Receptors, Corticotropin-Releasing Hormone, Biochemistry, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, medicine, Combinatorial Chemistry Techniques, Humans, Structure–activity relationship, Binding site, Isoquinoline, Receptor, Molecular Biology, Binding Sites, Molecular Structure, Depression, Aryl, Organic Chemistry, Antagonist, Isoquinolines, Receptor antagonist, chemistry, Drug Design, Molecular Medicine, hormones, hormone substitutes, and hormone antagonists
-
17
المؤلفون: William J. Zavadoski, Daniel R. Goldberg, Patricia-Ann Bourassa, Nicole Barucci, Stéphane De Lombaert, Qing Zhang, Robert J. Aiello, Jeffrey Dubins, Vishwas Paralkar
المصدر: 4.3 Pulmonary Circulation and Pulmonary Vascular Disease.
مصطلحات موضوعية: medicine.medical_specialty, Lung, TPH1, business.industry, Tryptophan hydroxylase, Mast cell, In vitro, chemistry.chemical_compound, medicine.anatomical_structure, Endocrinology, chemistry, Internal medicine, medicine, Serotonin, business, Perfusion, Histamine
-
18
المؤلفون: Frank Burkamp, Kevin J. Hodgetts, Rajagopal Bakthavatchalam, Robert Clarkson, Hutchison Alan J, Stéphane De Lombaert, Daniel N. Cortright, A. Brian Jones, Charles A. Blum, Peter Blurton, Harry Brielmann, Xiaozhang Zheng, Jayaraman Chandrasekhar, Marci Crandall
المصدر: Bioorganic & Medicinal Chemistry Letters. 16:5217-5221
مصطلحات موضوعية: Stereochemistry, Clinical Biochemistry, Molecular Conformation, TRPV1, Administration, Oral, Biological Availability, Pain, TRPV Cation Channels, Pharmaceutical Science, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Quinazoline, Animals, Humans, Urea, Structure–activity relationship, Molecular Biology, Chemistry, Aryl, Organic Chemistry, Antagonist, Analgesics, Non-Narcotic, Amides, Rats, Bioavailability, Piperazine, Solubility, Quinazolines, Molecular Medicine, Bioisostere
-
19
المؤلفون: Charles A. Blum, Stéphane De Lombaert, Xiaozhang Zheng
المصدر: Journal of Medicinal Chemistry. 47:2318-2325
مصطلحات موضوعية: Patch-Clamp Techniques, Stereochemistry, medicine.drug_class, hERG, Carboxamide, In Vitro Techniques, Chemical synthesis, Cell Line, Rats, Sprague-Dawley, Radioligand Assay, Structure-Activity Relationship, chemistry.chemical_compound, Drug Stability, Cyclohexanes, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Trifluoromethyl, biology, Imidazoles, Neuropeptide Y receptor, Amides, Small molecule, Potassium channel, Rats, Receptors, Neuropeptide Y, chemistry, Drug Design, Microsomes, Liver, biology.protein, Molecular Medicine
-
20
المؤلفون: Stéphane De Lombaert, Jianhua Huang, Andrzej Kieltyka, Renee Primus, Yoon Taeyoung, Michael Gulianello, Kevin J. Hodgetts, Dario Doller, Robbin Brodbeck
المصدر: Bioorganic & Medicinal Chemistry Letters. 13:2497-2500
مصطلحات موضوعية: Chemical Phenomena, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, In Vitro Techniques, Receptors, Corticotropin-Releasing Hormone, Biochemistry, Chemical synthesis, Structure-Activity Relationship, chemistry.chemical_compound, Microsomes, Drug Discovery, Structure–activity relationship, Humans, Receptor, Molecular Biology, Chemistry, Physical, Aryl, Organic Chemistry, Crf1 receptor, General Medicine, Combinatorial chemistry, In vitro, Pyrimidines, chemistry, Drug Design, Benzene derivatives, CNS agents, Lactam, Molecular Medicine, Indicators and Reagents