Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs von Sun, Hao, Piotrowski, David W, Orr, Suvi T M, Warmus, Joseph S, Wolford, Angela C, Coffey, Steven B, Futatsugi, Kentaro, Zhang, Yinsheng, Vaz, Alfin D N

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Synthesis of Small 3‑Fluoro- and 3,3-Difluoropyrrolidines Using Azomethine Ylide Chemistry von McAlpine, Indrawan, Tran-Dubé, Michelle, Wang, Fen, Scales, Stephanie, Matthews, Jean, Collins, Michael R, Nair, Sajiv K, Nguyen, Mary, Bian, Jianwei, Alsina, Luis Martinez, Sun, Jianmin, Zhong, Jiaying, Warmus, Joseph S, O’Neill, Brian T

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The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901 von Barrett, Stephen D., Bridges, Alexander J., Dudley, David T., Saltiel, Alan R., Fergus, James H., Flamme, Cathlin M., Delaney, Amy M., Kaufman, Michael, LePage, Sophie, Leopold, Wilbur R., Przybranowski, Sally A., Sebolt-Leopold, Judith, Van Becelaere, Keri, Doherty, Annette M., Kennedy, Robert M., Marston, Dan, Howard, W. Allen, Smith, Yvonne, Warmus, Joseph S., Tecle, Haile

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Discovery of 2‑(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)‑yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for... von Ruggeri, Roger B, Buckbinder, Leonard, Bagley, Scott W, Carpino, Philip A, Conn, Edward L, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Kung, Daniel W, Orr, Suvi T. M, Qi, Yingmei, Rocke, Benjamin N, Smith, Aaron, Warmus, Joseph S, Zhang, Yan, Bowles, Daniel, Widlicka, Daniel W, Eng, Heather, Ryder, Tim, Sharma, Raman, Wolford, Angela, Okerberg, Carlin, Walters, Karen, Maurer, Tristan S, Zhang, Yanwei, Bonin, Paul D, Spath, Samantha N, Xing, Gang, Hepworth, David, Ahn, Kay, Kalgutkar, Amit S

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Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries von Londregan, Allyn T., Piotrowski, David W., Futatsugi, Kentaro, Warmus, Joseph S., Boehm, Markus, Carpino, Philip A., Chin, Janice E., Janssen, Ann M., Roush, Nicole S., Buxton, Joanne, Hinchey, Terri

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Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors von Bagal, Sharan K, Omoto, Kiyoyuki, Blakemore, David C, Bungay, Peter J, Bilsland, James G, Clarke, Philip J, Corbett, Matthew S, Cronin, Ciaran N, Cui, J. Jean, Dias, Rebecca, Flanagan, Neil J, Greasley, Samantha E, Grimley, Rachel, Johnson, Eric, Fengas, David, Kitching, Linda, Kraus, Michelle L, McAlpine, Indrawan, Nagata, Asako, Waldron, Gareth J, Warmus, Joseph S

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Delineating the Ligand–Receptor Interactions That Lead to Biased Signaling at the μ‑Opioid Receptor von Kelly, Brendan, Hollingsworth, Scott A., Blakemore, David C., Owen, Robert M., Storer, R. Ian, Swain, Nigel A., Aydin, Deniz, Torella, Rubben, Warmus, Joseph S., Dror, Ron O.

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Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865) von Owen, Robert M, Blakemore, David, Cao, Lishuang, Flanagan, Neil, Fish, Rebecca, Gibson, Karl R, Gurrell, Rachel, Huh, Chan Woo, Kammonen, Juha, Mortimer-Cassen, Elisabeth, Nickolls, Sarah A, Omoto, Kiyoyuki, Owen, Dafydd, Pike, Andy, Pryde, David C, Reynolds, David S, Roeloffs, Rosemarie, Rose, Colin, Stead, Clara, Takeuchi, Mifune, Warmus, Joseph S, Watson, Christine

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Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents von Londregan, Allyn T, Wei, Liuqing, Xiao, Jun, Lintner, Nathanael G, Petersen, Donna, Dullea, Robert G, McClure, Kim F, Bolt, Michael W, Warmus, Joseph S, Coffey, Steven B, Limberakis, Chris, Genovino, Julien, Thuma, Benjamin A, Hesp, Kevin D, Aspnes, Gary E, Reidich, Benjamin, Salatto, Christopher T, Chabot, Jeffrey R, Cate, Jamie H. D, Liras, Spiros, Piotrowski, David W

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Design and Identification of a Novel, Functionally Subtype Selective GABA A Positive Allosteric Modulator (PF-06372865) von Owen, Robert M, Blakemore, David, Cao, Lishuang, Flanagan, Neil, Fish, Rebecca, Gibson, Karl R, Gurrell, Rachel, Huh, Chan Woo, Kammonen, Juha, Mortimer-Cassen, Elisabeth, Nickolls, Sarah A, Omoto, Kiyoyuki, Owen, Dafydd, Pike, Andy, Pryde, David C, Reynolds, David S, Roeloffs, Rosemarie, Rose, Colin, Stead, Clara, Takeuchi, Mifune, Warmus, Joseph S, Watson, Christine

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Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain von Bagal, Sharan K, Andrews, Mark, Bechle, Bruce M, Bian, Jianwei, Bilsland, James, Blakemore, David C, Braganza, John F, Bungay, Peter J, Corbett, Matthew S, Cronin, Ciaran N, Cui, Jingrong Jean, Dias, Rebecca, Flanagan, Neil J, Greasley, Samantha E, Grimley, Rachel, James, Kim, Johnson, Eric, Kitching, Linda, Kraus, Michelle L, McAlpine, Indrawan, Nagata, Asako, Ninkovic, Sacha, Omoto, Kiyoyuki, Scales, Stephanie, Skerratt, Sarah E, Sun, Jianmin, Tran-Dubé, Michelle, Waldron, Gareth J, Wang, Fen, Warmus, Joseph S

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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes von Storer, R. Ian, Pike, Andy, Swain, Nigel A., Alexandrou, Aristos J., Bechle, Bruce M., Blakemore, David C., Brown, Alan D., Castle, Neil A., Corbett, Matthew S., Flanagan, Neil J., Fengas, David, Johnson, M. Scott, Jones, Lyn H., Marron, Brian E., Payne, C. Elizabeth, Printzenhoff, David, Rawson, David J., Rose, Colin R., Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W., Torella, Rubben, Tseng, Elaine, Warmus, Joseph S.

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Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections von Brown, Matthew F, Reilly, Usa, Abramite, Joseph A, Arcari, Joel T, Oliver, Robert, Barham, Rose A, Che, Ye, Chen, Jinshan Michael, Collantes, Elizabeth M, Chung, Seung Won, Desbonnet, Charlene, Doty, Jonathan, Doroski, Matthew, Engtrakul, Juntyma J, Harris, Thomas M, Huband, Michael, Knafels, John D, Leach, Karen L, Liu, Shenping, Marfat, Anthony, Marra, Andrea, McElroy, Eric, Melnick, Michael, Menard, Carol A, Montgomery, Justin I, Mullins, Lisa, Noe, Mark. C, O’Donnell, John, Penzien, Joseph, Plummer, Mark S, Price, Loren M, Shanmugasundaram, Veerabahu, Thoma, Christy, Uccello, Daniel P, Warmus, Joseph S, Wishka, Donn G

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The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain von Brown, Alan D., Bagal, Sharan K., Blackwell, Paul, Blakemore, David C., Brown, Bruce, Bungay, Peter J., Corless, Martin, Crawforth, James, Fengas, David, Fenwick, David R., Gray, Victoria, Kemp, Mark, Klute, Wolfgang, Malet Sanz, Laia, Miller, Duncan, Murata, Yoshihisa, Payne, C. Elizabeth, Skerratt, Sarah, Stevens, Edward B., Warmus, Joseph S.

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One-Pot Synthesis of α‑Branched N‑Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics von Dai, Chunhui, Genovino, Julien, Bechle, Bruce M, Corbett, Matthew S, Huh, Chan Woo, Rose, Colin R, Sun, Jianmin, Warmus, Joseph S, Blakemore, David C

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Discovery of a Series of Indazole TRPA1 Antagonists von Pryde, David C, Marron, Brian E, West, Christopher W, Reister, Steven, Amato, George, Yoger, Katrina, Antonio, Brett, Padilla, Karen, Cox, Peter J, Turner, Jamie, Warmus, Joseph S, Swain, Nigel A, Omoto, Kiyoyuki, Mahoney, John H, Gerlach, Aaron C

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Diastereoselective Synthesis of β‑Heteroaryl syn-α-Methyl-β-Amino Acid Derivatives via a Double Chiral Auxiliary Approach von Bian, Jianwei, Blakemore, David, Warmus, Joseph S, Sun, Jianmin, Corbett, Matthew, Rose, Colin R, Bechle, Bruce M

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2-Alkylamino-and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase... von WARMUS, Joseph S, FLAMME, Cathlin, MERRIMAN, Ronald, OHREN, Jeffrey, PAVLOVSKY, Alexander, PRZYBRANOWSKI, Sally, TECLE, Haile, VALIK, Heather, WHITEHEAD, Christopher, ERLI ZHANG, LU YAN ZHANG, BARRETT, Stephen, BRIDGES, Alexander, HUIFEN CHEN, GOWAN, Richard, KAUFMAN, Michael, SEBOLT-LEOPOLD, Judy, LEOPOLD, Wilbur

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Design and development of histone deacetylase (HDAC) chemical probes for cell-based profiling von Albrow, Victoria E, Grimley, Rachel L, Clulow, James, Rose, Colin R, Sun, Jianmin, Warmus, Joseph S, Tate, Edward W, Jones, Lyn H, Storer, R. Ian

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Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC von Warmus, Joseph S., Quinn, Cheryl L., Taylor, Clarke, Murphy, Sean T., Johnson, Timothy A., Limberakis, Chris, Ortwine, Daniel, Bronstein, Joel, Pagano, Paul, Knafels, John D., Lightle, Sandra, Mochalkin, Igor, Brideau, Roger, Podoll, Terry

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