未登录 The state of the art in secondary pharmacology and its impact on the safety of new medicines (May, 10.1038/s41573-024-00942-3, 2024) 次要药理学的最新技术及其对新药安全性的影响 (10.1038/s41573-024-00942-3，2024 5月) Brennan, Richard J.; Jenkinson, Stephen; Brown, Andrew; Delaunois, Annie; Dumotier, Berengere; Pannirselvam, Malar; Rao, Mohan; Ribeiro, Lyn Rosenbrier; Schmidt, Friedemann; Sibony, Alicia; Timsit, Yoav; Sales, Vicencia Toledo; Armstrong, Duncan; Lagrutta, Armando; Mittlestadt, Scott W.; Naven, Russell; Peri, Ravikumar; Roberts, Sonia; Vergis, James M.; Valentin, Jean-Pierre 分享 收藏
The state of the art in secondary pharmacology and its impact on the safety of new medicines 二级药理学的最新技术及其对新药安全性的影响 Brennan, Richard J.; Jenkinson, Stephen; Brown, Andrew; Delaunois, Annie; Dumotier, Berengere; Pannirselvam, Malar; Rao, Mohan; Ribeiro, Lyn Rosenbrier; Schmidt, Friedemann; Sibony, Alicia; Timsit, Yoav; Sales, Vicencia Toledo; Armstrong, Duncan; Lagrutta, Armando; Mittlestadt, Scott W.; Naven, Russell; Peri, Ravikumar; Roberts, Sonia; Vergis, James M.; Valentin, Jean-Pierre 分享 收藏
Comprehensive Nonclinical Safety Assessment of Nirmatrelvir Supporting Timely Development of the SARS-COV-2 Antiviral Therapeutic, Paxlovid™ Sathish, Jean G.; Bhatt, Siddhartha; DaSilva, Jamie K.; Flynn, Declan; Jenkinson, Stephen; Kalgutkar, Amit S.; Liu, Maggie; Manickam, Balasubramanian; Pinkstaff, Jason; Reagan, William J.; Shirai, Norimitsu; Shoieb, Ahmed M.; Sirivelu, Madhu; Vispute, Saurabh; Vitsky, Allison; Walters, Karen; Wisialowski, Todd A.; Updyke, Lawrence W. 分享 收藏
Characterization of a high throughput human stem cell cardiomyocyte assay to predict drug-induced changes in clinical electrocardiogram parameters Kilfoil, Peter; Feng, Shuyun Lily; Bassyouni, Asser; Lee, Tiffany; Leishman, Derek; Li, Dingzhou; MacEwan, David J.; Sharma, Parveen; Watt, Eric D.; Jenkinson, Stephen 分享 收藏
Time for a Fully Integrated Nonclinical-Clinical Risk Assessment to Streamline QT Prolongation Liability Determinations: A Pharma Industry Perspective Vargas, Hugo M.; Rolf, Michael G.; Wisialowski, Todd A.; Achanzar, William; Bahinski, Anthony; Bass, Alan; Benson, Charles T.; Chaudhary, Khuram W.; Couvreur, Nicolas; Dota, Corina; Engwall, Michael J.; Michael Foley, C.; Gallacher, David; Greiter-Wilke, Andrea; Guillon, Jean-Michel; Guth, Brian; Himmel, Herbert M.; Hegele-Hartung, Christa; Ito, Maki; Jenkinson, Stephen; Chiba, Katsuyoshi; Lagrutta, Armando; Levesque, Paul; Martel, Eric; Okai, Yoshiko; Peri, Ravikumar; Pointon, Amy; Qu, Yusheng; Teisman, Ard; Traebert, Martin; Yoshinaga, Takashi; Gintant, Gary A.; Leishman, Derek J.; Valentin, Jean-Pierre 分享 收藏
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H1 Receptor Inverse Agonist Lall, Manjinder S.; Bassyouni, Asser; Bradow, James; Brown, Maria; Bundesmann, Mark; Chen, Jinshan; Ciszewski, Gregory; Hagen, Anne E.; Hyek, Dennis; Jenkinson, Stephen; Liu, Bo; Obach, R. Scott; Pan, Senliang; Reilly, Usa; Sach, Neal; Smaltz, Daniel J.; Spracklin, Douglas K.; Starr, Jeremy; Wagenaar, Melissa; Walker, Gregory S. 分享 收藏
Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response (vol 10, 4075, 2019) Benredjem, Besma; Gallion, Jonathan; Pelletier, Dennis; Dallaire, Paul; Charbonneau, Johanie; Cawkill, Darren; Nagi, Karim; Gosink, Mark; Lukasheva, Viktoryia; Jenkinson, Stephen; Ren, Yong; Somps, Christopher; Murat, Brigitte; van der Westhuizen, Emma; Le Gouill, Christian; Lichtarge, Olivier; Schmidt, Anne; Bouvier, Michel; Pineyro, Graciela 分享 收藏
Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response Benredjem, Besma; Gallion, Jonathan; Pelletier, Dennis; Dallaire, Paul; Charbonneau, Johanie; Cawkill, Darren; Nagi, Karim; Gosink, Mark; Lukasheva, Viktoryia; Jenkinson, Stephen; Ren, Yong; Somps, Christopher; Murat, Brigitte; Van Der Westhuizen, Emma; Le Gouill, Christian; Lichtarge, Olivier; Schmidt, Anne; Bouvier, Michel; Pineyro, Graciela 分享 收藏
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Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1 Humphrey, John M.; Movsesian, Matthew; Ende, Christopher W. Am; Becker, Stacey L.; Chappie, Thomas A.; Jenkinson, Stephen; Liras, Jennifer L.; Liras, Spiros; Orozco, Christine; Pandit, Jayvardhan; Vajdos, Felix F.; Vandeput, Fabrice; Yang, Eddie; Menniti, Frank S. 分享 收藏
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Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189 晚期微粒体氧化减少药物-药物相互作用并鉴定磷酸二酯酶2A抑制剂PF-06815189 Stepan, Antonia F.; Tran, Tuan P.; Helal, Christopher J.; Brown, Maria S.; Chang, Cheng; O'Connor, Rebecca E.; De Vivo, Michael; Doran, Shawn D.; Fisher, Ethan L.; Jenkinson, Stephen; Karanian, David; Kormos, Bethany L.; Sharma, Raman; Walker, Gregory S.; Wright, Ann S.; Yang, Edward X.; Brodney, Michael A.; Wager, Travis T.; Verhoest, Patrick R.; Obach, R. Scott 分享 收藏
Design and Synthesis of γ- and δ-Lactarn M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity Davoren, Jennifer E.; Garney, Michelle; Pettersen, Betty; Brodney, Michael A.; Edgerton, Jeremy R.; Fortin, Jean-Philippe; Grimwood, Sarah; Harris, Anthony R.; Jenkinson, Stephen; Kenakin, Terry; Lazzaro, John T.; Lee, Che-Wah; Lotarski, Susan M.; Nottebaum, Lisa; O'Neil, Steven V.; Popiolek, Michael; Ramsey, Simeon; Steyn, Stefanus J.; Thorn, Catherine A.; Zhang, Lei; Webb, Damien 分享 收藏
Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A Quinlan, Casey L.; Kaiser, Stephen E.; Bolanos, Ben; Nowlin, Dawn; Grantner, Rita; Karlicek-Bryant, Shannon; Feng, Jun Li; Jenkinson, Stephen; Freeman-Cook, Kevin; Dann, Stephen G.; Wang, Xiaoli; Wells, Peter A.; Fantin, Valeria R.; Stewart, Al E.; Grant, Stephan K. 分享 收藏
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects Davoren, Jennifer E.; Lee, Che-Wah; Garnsey, Michelle; Brodney, Michael A.; Cordes, Jason; Dlugolenski, Keith; Edgerton, Jeremy R.; Harris, Anthony R.; Helal, Christopher J.; Jenkinson, Stephen; Kauffman, Gregory W.; Kenakin, Terrence P.; Lazzaro, John T.; Lotarski, Susan M.; Mao, Yuxia; Nason, Deane M.; Northcott, Carrie; Nottebaum, Lisa; O'Neil, Steven V.; Pettersen, Betty; Popiolek, Michael; Reinhart, Veronica; Salomon-Ferrer, Romelia; Steyn, Stefanus J.; Webb, Damien; Zhang, Lei; Grimwood, Sarah 分享 收藏
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists Rouquet, Guy; Moore, Dianna E.; Spain, Malcolm; Allwood, Daniel M.; Battilocchio, Claudio; Blakemore, David C.; Fish, Paul V.; Jenkinson, Stephen; Jessiman, Alan S.; Ley, Steven V.; McMurray, Gordon; Storer, R. Ian 分享 收藏
Blockade of X4-Tropic HIV-1 Cellular Entry by GSK812397, a Potent Noncompetitive CXCR4 Receptor Antagonist Jenkinson, Stephen; Thomson, Michael; McCoy, David; Edelstein, Mark; Danehower, Susan; Lawrence, Wendell; Wheelan, Pat; Spaltenstein, Andrew; Gudmundsson, Kristjan 分享 收藏
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules Briscoe, Celia P.; Peat, Andrew J.; McKeown, Stephen C.; Corbett, David F.; Goetz, Aaron S.; Littleton, Thomas R.; McCoy, David C.; Kenakin, Terry P.; Andrews, John L.; Ammala, Carina; Fornwald, James A.; Ignar, Diane M.; Jenkinson, Stephen 分享 收藏
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