Discovery and Preclinical Profiling of 3‑[4-(Morpholin-4-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-5-yl]benzonitrile (PF-06447475), a Highly Potent, Selective, Brain Penetrant, and in Vivo Ac... von Henderson, Jaclyn L., Kormos, Bethany L., Hayward, Matthew M., Coffman, Karen J., Jasti, Jayasankar, Kurumbail, Ravi G., Wager, Travis T., Verhoest, Patrick R., Noell, G. Stephen, Chen, Yi, Needle, Elie, Berger, Zdenek, Steyn, Stefanus J., Houle, Christopher, Hirst, Warren D., Galatsis, Paul

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Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes von Wager, Travis T, Chandrasekaran, Ramalakshmi Y, Hou, Xinjun, Troutman, Matthew D, Verhoest, Patrick R, Villalobos, Anabella, Will, Yvonne

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A Novel Mechanism Controlling Resetting Speed of the Circadian Clock to Environmental Stimuli von Pilorz, Violetta, Cunningham, Peter S., Jackson, Anthony, West, Alexander C., Wager, Travis T., Loudon, Andrew S.I., Bechtold, David A.

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Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes von Meng, Qing-Jun, Maywood, Elizabeth S., Bechtold, David A., Lu, Wei-Qun, Li, Jian, Gibbs, Julie E., Dupré, Sandrine M., Chesham, Johanna E., Rajamohan, Francis, Knafels, John, Sneed, Blossom, Zawadzke, Laura E., Ohren, Jeffrey F., Walton, Kevin M., Wager, Travis T., Hastings, Michael H., Loudon, Andrew S. I., Takahashi, Joseph S.

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Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties von Wager, Travis T, Hou, Xinjun, Verhoest, Patrick R, Villalobos, Anabella

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Quantitative Assessment of the Impact of Fluorine Substitution on P‑Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability von Pettersson, Martin, Hou, Xinjun, Kuhn, Max, Wager, Travis T, Kauffman, Gregory W, Verhoest, Patrick R

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Design, Optimization, and Study of Small Molecules That Target Tau Pre-mRNA and Affect Splicing von Chen, Jonathan L, Zhang, Peiyuan, Abe, Masahito, Aikawa, Haruo, Zhang, Liying, Frank, Alexander J, Zembryski, Timothy, Hubbs, Christopher, Park, HaJeung, Withka, Jane, Steppan, Claire, Rogers, Lucy, Cabral, Shawn, Pettersson, Martin, Wager, Travis T, Fountain, Matthew A, Rumbaugh, Gavin, Childs-Disney, Jessica L, Disney, Matthew D

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Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a... von Zhang, Lei, Villalobos, Anabella, Beck, Elizabeth M, Bocan, Thomas, Chappie, Thomas A, Chen, Laigao, Grimwood, Sarah, Heck, Steven D, Helal, Christopher J, Hou, Xinjun, Humphrey, John M, Lu, Jiemin, Skaddan, Marc B, McCarthy, Timothy J, Verhoest, Patrick R, Wager, Travis T, Zasadny, Kenneth

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In Vitro–In Vivo Extrapolation of Key Transporter Activity at the Blood–Brain Barrier von Trapa, Patrick E., Troutman, Matthew D., Lau, Thomas Y., Wager, Travis T., Maurer, Tristan S., Patel, Nandini C., West, Mark A., Umland, John P., Carlo, Anthony A., Feng, Bo, Liras, Jennifer L.

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Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs von Ferruz, Noelia, Doerr, Stefan, Vanase-Frawley, Michelle A., Zou, Yaozhong, Chen, Xiaomin, Marr, Eric S., Nelson, Robin T., Kormos, Bethany L., Wager, Travis T., Hou, Xinjun, Villalobos, Anabella, Sciabola, Simone, De Fabritiis, Gianni

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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE von Seneviratne, Uthpala, Huang, Zhen, am Ende, Christopher W., Butler, Todd W., Cleary, Leah, Dresselhaus, Erica, Evrard, Edelweiss, Fisher, Ethan L., Green, Michael E., Helal, Christopher J., Humphrey, John M., Lanyon, Lorraine F., Marconi, Michael, Mukherjee, Paramita, Sciabola, Simone, Steppan, Claire M., Sylvain, Emily K., Tuttle, Jamison B., Verhoest, Patrick R., Wager, Travis T., Xie, Longfei, Ramaswamy, Gayathri, Johnson, Douglas S., Pettersson, Martin

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Selective Inhibition of Casein Kinase 1ϵ Minimally Alters Circadian Clock Period von Walton, Kevin M., Fisher, Katherine, Rubitski, David, Marconi, Michael, Meng, Qing-Jun, Sládek, Martin, Adams, Jessica, Bass, Michael, Chandrasekaran, Rama, Butler, Todd, Griffor, Matt, Rajamohan, Francis, Serpa, Megan, Chen, Yuhpyng, Claffey, Michelle, Hastings, Michael, Loudon, Andrew, Maywood, Elizabeth, Ohren, Jeffrey, Doran, Angela, Wager, Travis T.

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Improving the Odds of Success in Drug Discovery: Choosing the Best Compounds for in Vivo Toxicology Studies von Wager, Travis T, Kormos, Bethany L, Brady, Joseph T, Will, Yvonne, Aleo, Michael D, Stedman, Donald B, Kuhn, Max, Chandrasekaran, Ramalakshmi Y

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Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity von Cunningham, Peter S., Ahern, Siobhán A., Smith, Laura C., da Silva Santos, Carla S., Wager, Travis T., Bechtold, David A.

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Harnessing Preclinical Data as a Predictive Tool for Human Brain Tissue Targeting von Patel, Nandini C, Feng, Bo, Hou, Xinjun, West, Mark A, Trapa, Patrick E, Sciabola, Simone, Verhoest, Patrick, Liras, Jennifer L, Maurer, Tristan S, Wager, Travis T

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Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids von Bryant, Camron D, Parker, Clarissa C, Zhou, Lili, Olker, Christopher, Chandrasekaran, Ramalakshmi Y, Wager, Travis T, Bolivar, Valerie J, Loudon, Andrew S, Vitaterna, Martha H, Turek, Fred W, Palmer, Abraham A

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Author Correction: Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs von Ferruz, Noelia, Doerr, Stefan, Vanase-Frawley, Michelle A., Zou, Yaozhong, Chen, Xiaomin, Marr, Eric S., Nelson, Robin T., Kormos, Bethany L., Wager, Travis T., Hou, Xinjun, Villalobos, Anabella, Sciabola, Simone, De Fabritiis, Gianni

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A Direct and Mild Conversion of Tertiary Aryl Amides to Methyl Esters Using Trimethyloxonium Tetrafluoroborate: A Very Useful Complement to Directed Metalation Reactions von Keck, Gary E, McLaws, Mark D, Wager, Travis T

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Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold von Galatsis, Paul, Henderson, Jaclyn L., Kormos, Bethany L., Han, Seungil, Kurumbail, Ravi G., Wager, Travis T., Verhoest, Patrick R., Noell, G. Stephen, Chen, Yi, Needle, Elie, Berger, Zdenek, Steyn, Stefanus J., Houle, Christopher, Hirst, Warren D.

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Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors von Wager, Travis T, Galatsis, Paul, Chandrasekaran, Ramalakshmi Y, Butler, Todd W, Li, Jianke, Zhang, Lei, Mente, Scot, Subramanyam, Chakrapani, Liu, Shenping, Doran, Angela C, Chang, Cheng, Fisher, Katherine, Grimwood, Sarah, Hedde, Joseph R, Marconi, Michael, Schildknegt, Klaas

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