Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition
Chappie, Thomas A, Helal, Christopher J, Hou, Xinjun
Published in Journal of medicinal chemistry (13.09.2012)
Published in Journal of medicinal chemistry (13.09.2012)
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High‐Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates
Clement, Helen A., Boghi, Michele, McDonald, Rory M., Bernier, Louise, Coe, Jotham W., Farrell, William, Helal, Christopher J., Reese, Matthew R., Sach, Neal W., Lee, Jack C., Hall, Dennis G.
Published in Angewandte Chemie International Edition (16.12.2019)
Published in Angewandte Chemie International Edition (16.12.2019)
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Synthetic Approaches to New Drugs Approved during 2018
Flick, Andrew C, Leverett, Carolyn A, Ding, Hong X, McInturff, Emma, Fink, Sarah J, Helal, Christopher J, DeForest, Jacob C, Morse, Peter D, Mahapatra, Subham, O’Donnell, Christopher J
Published in Journal of medicinal chemistry (08.10.2020)
Published in Journal of medicinal chemistry (08.10.2020)
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Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy
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Published in Journal of medicinal chemistry (24.12.2009)
Published in Journal of medicinal chemistry (24.12.2009)
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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation
McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
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Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs
Walsky, Robert L, Obach, R Scott, Hyland, Ruth, Kang, Ping, Zhou, Sue, West, Michael, Geoghegan, Kieran F, Helal, Christopher J, Walker, Gregory S, Goosen, Theunis C, Zientek, Michael A
Published in Drug metabolism and disposition (01.09.2012)
Published in Drug metabolism and disposition (01.09.2012)
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The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging
Zhang, Lei, Chen, Laigao, Beck, Elizabeth M, Chappie, Thomas A, Coelho, Richard V, Doran, Shawn D, Fan, Kuo-Hsien, Helal, Christopher J, Humphrey, John M, Hughes, Zoe, Kuszpit, Kyle, Lachapelle, Erik A, Lazzaro, John T, Lee, Chewah, Mather, Robert J, Patel, Nandini C, Skaddan, Marc B, Sciabola, Simone, Verhoest, Patrick R, Young, Joseph M, Zasadny, Kenneth, Villalobos, Anabella
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor
Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
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Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
Kleiman, Robin J, Chapin, Douglas S, Christoffersen, Curt, Freeman, Jody, Fonseca, Kari R, Geoghegan, Kieran F, Grimwood, Sarah, Guanowsky, Victor, Hajós, Mihály, Harms, John F, Helal, Christopher J, Hoffmann, William E, Kocan, Geralyn P, Majchrzak, Mark J, McGinnis, Dina, McLean, Stafford, Menniti, Frank S, Nelson, Fredrick, Roof, Robin, Schmidt, Anne W, Seymour, Patricia A, Stephenson, Diane T, Tingley, Francis David, Vanase-Frawley, Michelle, Verhoest, Patrick R, Schmidt, Christopher J
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
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Journal Article
High‐Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates
Clement, Helen A., Boghi, Michele, McDonald, Rory M., Bernier, Louise, Coe, Jotham W., Farrell, William, Helal, Christopher J., Reese, Matthew R., Sach, Neal W., Lee, Jack C., Hall, Dennis G.
Published in Angewandte Chemie (16.12.2019)
Published in Angewandte Chemie (16.12.2019)
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Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides
Zhou, Hua, Mukherjee, Paramita, Liu, Rongqiang, Evrard, Edelweiss, Wang, Dianpeng, Humphrey, John M, Butler, Todd W, Hoth, Lise R, Sperry, Jeffrey B, Sakata, Sylvie K, Helal, Christopher J, am Ende, Christopher W
Published in Organic letters (02.02.2018)
Published in Organic letters (02.02.2018)
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Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease
Helal, Christopher J., Sanner, Mark A., Cooper, Christopher B., Gant, Thomas, Adam, Mavis, Lucas, John C., Kang, Zhijun, Kupchinsky, Stanley, Ahlijanian, Michael K., Tate, Bonnie, Menniti, Frank S., Kelly, Kristin, Peterson, Marcia
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
Published in Bioorganic & medicinal chemistry letters (15.11.2004)
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Synthetic Approaches to the New Drugs Approved During 2017
Flick, Andrew C, Leverett, Carolyn A, Ding, Hong X, McInturff, Emma, Fink, Sarah J, Helal, Christopher J, O’Donnell, Christopher J
Published in Journal of medicinal chemistry (22.08.2019)
Published in Journal of medicinal chemistry (22.08.2019)
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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 Novel Phosphodiesterase 2A PET Ligand
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
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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5‑Aryltetrazoles from Direct C–H Arylation with Aryl Bromides
Zhang, Yuan, Lee, Jack Chang Hung, Reese, Matthew R, Boscoe, Brian P, Humphrey, John M, Helal, Christopher J
Published in Journal of organic chemistry (17.04.2020)
Published in Journal of organic chemistry (17.04.2020)
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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
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis
Himmelbauer, Martin K., Bajrami, Bekim, Basile, Rebecca, Capacci, Andrew, Chen, TeYu, Choi, Colin K., Gilfillan, Rab, Gonzalez-Lopez de Turiso, Felix, Gu, Chungang, Hoemberger, Marc, Johnson, Douglas S., Jones, J. Howard, Kadakia, Ekta, Kirkland, Melissa, Lin, Edward Y., Liu, Ying, Ma, Bin, Magee, Tom, Mantena, Srinivasa, Marx, Isaac E., Metrick, Claire M., Mingueneau, Michael, Murugan, Paramasivam, Muste, Cathy A., Nadella, Prasad, Nevalainen, Marta, Parker Harp, Chelsea R., Pattaropong, Vatee, Pietrasiewicz, Alicia, Prince, Robin J., Purgett, Thomas J., Santoro, Joseph C., Schulz, Jurgen, Sciabola, Simone, Tang, Hao, Vandeveer, H. George, Wang, Ti, Yousaf, Zain, Helal, Christopher J., Hopkins, Brian T.
Published in Journal of medicinal chemistry (23.05.2024)
Published in Journal of medicinal chemistry (23.05.2024)
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Discovery of Clinical Candidate PF-06648671: A Potent γ‑Secretase Modulator for the Treatment of Alzheimer’s Disease
Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., am Ende, Christopher W., Butler, Todd W., Dorff, Peter H., Efremov, Ivan V., Evrard, Edelweiss, Green, Michael E., Helal, Christopher J., Kauffman, Gregory W., Mullins, Patrick B., Navaratnam, Thayalan, O’Donnell, Christopher J., O’Sullivan, Theresa J., Patel, Nandini C., Stepan, Antonia F., Stiff, Cory M., Subramanyam, Chakrapani, Trapa, Patrick, Tran, Tuan P., Vetelino, Beth Cooper, Yang, Eddie, Xie, Longfei, Pustilnik, Leslie R., Steyn, Stefanus J., Wood, Kathleen M., Bales, Kelly R., Hajos-Korcsok, Eva, Verhoest, Patrick R.
Published in Journal of medicinal chemistry (27.06.2024)
Published in Journal of medicinal chemistry (27.06.2024)
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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE
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
Published in Cell chemical biology (18.02.2021)
Published in Cell chemical biology (18.02.2021)
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