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Pharmacologic characterization of atogepant: A potent and selective calcitonin gene–related peptide receptor antagonist
Moore, Eric, Bell, Ian M, Fraley, Mark E, Burgey, Christopher S, White, Rebecca B, Li, Chi-Chung, Regan, Christopher P, Danziger, Andrew, McGaraughty, Steve P, Naseri Kouzehgarani, Ghazal, Salvatore, Christopher, Banerjee, Pradeep
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A novel glucosylceramide synthase inhibitor attenuates alpha synuclein pathology and lysosomal dysfunction in preclinical models of synucleinopathy
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Published in Neurobiology of disease (01.11.2021)
Published in Neurobiology of disease (01.11.2021)
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Invention of novel 3-aminopiperidin-2-ones as calcitonin gene-related peptide receptor antagonists
Staas, Donnette D., Bell, Ian M., Burgey, Christopher S., Deng, James Z., Gallicchio, Steven N., Lim, John J., Paone, Daniel V., Potteiger, Craig M., Shaw, Anthony W., Stevenson, Heather, Stump, Craig A., Blair Zartman, C., Moore, Eric L., Bruno, Joseph G., Mosser, Scott D., White, Rebecca B., Kane, Stefanie A., Salvatore, Christopher A., Graham, Samuel L., Williams, Theresa M., Selnick, Harold G., Fraley, Mark E.
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Published in Bioorganic & medicinal chemistry letters (01.11.2024)
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Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer
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Published in Journal of medicinal chemistry (24.07.2008)
Published in Journal of medicinal chemistry (24.07.2008)
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Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections
Loughran, H. Marie, Schirripa, Kathy M., Roecker, Anthony J., Breslin, Michael J., Tong, Ling, Fillgrove, Kerry L., Kuo, Yuhsin, Bleasby, Kelly, Collier, Hannah, Altman, Michael D., Ford, Melissa C., Newman, Justin A., Drolet, Robert E., Cosden, Mali, Jinn, Sarah, Flick, Rosemarie B., Liu, Xiaomei, Minnick, Christina, Watt, Marla L., Lemaire, Wei, Burlein, Christine, Adam, Gregory C., Austin, Lauren A., Marcus, Jacob N., Smith, Sean M., Fraley, Mark E.
Published in ACS medicinal chemistry letters (11.01.2024)
Published in ACS medicinal chemistry letters (11.01.2024)
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Discovery of 5′′-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia
Roecker, Anthony J., Mercer, Swati P., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Steen, Justin T., Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.
Published in ChemMedChem (01.02.2014)
Published in ChemMedChem (01.02.2014)
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Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson’s Disease
Roecker, Anthony J., Schirripa, Kathy M., Loughran, H. Marie, Tong, Ling, Liang, Tao, Fillgrove, Kerry L., Kuo, Yuhsin, Bleasby, Kelly, Collier, Hannah, Altman, Michael D., Ford, Melissa C., Drolet, Robert E., Cosden, Mali, Jinn, Sarah, Hatcher, Nathan G., Yao, Lihang, Kandebo, Monika, Vardigan, Joshua D., Flick, Rosemarie B., Liu, Xiaomei, Minnick, Christina, Price, Laura A., Watt, Marla L., Lemaire, Wei, Burlein, Christine, Adam, Gregory C., Austin, Lauren A., Marcus, Jacob N., Smith, Sean M., Fraley, Mark E.
Published in ACS medicinal chemistry letters (09.02.2023)
Published in ACS medicinal chemistry letters (09.02.2023)
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Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine
Crowley, Brendan M., Stump, Craig A., Nguyen, Diem N., Potteiger, Craig M., McWherter, Melody A., Paone, Daniel V., Quigley, Amy G., Bruno, Joseph G., Cui, Dan, Culberson, J. Christopher, Danziger, Andrew, Fandozzi, Christine, Gauvreau, Danny, Kemmerer, Amanda L., Menzel, Karsten, Moore, Eric L., Mosser, Scott D., Reddy, Vijay, White, Rebecca B., Salvatore, Christopher A., Kane, Stefanie A., Bell, Ian M., Selnick, Harold G., Fraley, Mark E., Burgey, Christopher S.
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
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An Inhibitor of the Kinesin Spindle Protein Activates the Intrinsic Apoptotic Pathway Independently of p53 and De Novo Protein Synthesis
Tao, Weikang, South, Victoria J., Diehl, Ronald E., Davide, Joseph P., Sepp-Lorenzino, Laura, Fraley, Mark E., Arrington, Kenneth L., Lobell, Robert B.
Published in Molecular and Cellular Biology (01.01.2007)
Published in Molecular and Cellular Biology (01.01.2007)
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Development of thioquinazolinones, allosteric Chk1 kinase inhibitors
Converso, Antonella, Hartingh, Timothy, Garbaccio, Robert M., Tasber, Edward, Rickert, Keith, Fraley, Mark E., Yan, Youwei, Kreatsoulas, Constantine, Stirdivant, Steve, Drakas, Bob, Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Mao, Xianzhi, Abrams, Marc T., Beck, Stephen C., Tao, Weikang, Lobell, Rob, Sepp-Lorenzino, Laura, Zugay-Murphy, Joan, Sardana, Vinod, Munshi, Sanjeev K., Jezequel-Sur, Sylvie Marie, Zuck, Paul D., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.02.2009)
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Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase
Converso, Antonella, Hartingh, Timothy, Fraley, Mark E., Garbaccio, Robert M., Hartman, George D., Huang, Shaei Y., Majercak, John M., McCampbell, Alexander, Na, Sang Jin, Ray, William J., Savage, Mary J., Wolffe, Carrie, Yeh, Suzie, Yu, Yuanjiang, White, Rebecca, Zhang, Rena
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Published in Bioorganic & medicinal chemistry letters (15.06.2014)
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3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts
Brnardic, Edward J., Fraley, Mark E., Garbaccio, Robert M., Layton, Mark E., Sanders, John M., Culberson, Chris, Jacobson, Marlene A., Magliaro, Brian C., Hutson, Pete H., O’Brien, Julie A., Huszar, Sarah L., Uslaner, Jason M., Fillgrove, Kerry L., Tang, Cuyue, Kuo, Yuhsin, Sur, Sylvie M., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
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Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates
Dudkin, Vadim Y., Rickert, Keith, Kreatsoulas, Constantine, Wang, Cheng, Arrington, Kenneth L., Fraley, Mark E., Hartman, George D., Yan, Yowei, Ikuta, Mari, Stirdivant, Steven M., Drakas, Robert A., Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Lobell, Robert B., Sepp-Lorenzino, Laura
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
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Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5- a]pyrimidines: A New Class of KDR Kinase Inhibitors
Fraley, Mark E., Hoffman, William F., Rubino, Robert S., Hungate, Randall W., Tebben, Andrew J., Rutledge, Ruth Z., McFall, Rosemary C., Huckle, William R., Kendall, Richard L., Coll, Kathleen E., Thomas, Kenneth A.
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
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Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors
Brnardic, Edward J., Garbaccio, Robert M., Fraley, Mark E., Tasber, Edward S., Steen, Justin T., Arrington, Kenneth L., Dudkin, Vadim Y., Hartman, George D., Stirdivant, Steven M., Drakas, Bob A., Rickert, Keith, Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Hardwick, James, Tao, Weikang, Beck, Stephen C., Mao, Xianzhi, Lobell, Robert B., Sepp-Lorenzino, Laura, Yan, Youwei, Ikuta, Mari, Munshi, Sanjeev K., Kuo, Lawrence C., Kreatsoulas, Constantine
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
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Kinesin spindle protein (KSP) inhibitors. Part V: Discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by β-fluorination to overcome cellular efflux by P-glycoprotein
Cox, Christopher D., Breslin, Michael J., Whitman, David B., Coleman, Paul J., Garbaccio, Robert M., Fraley, Mark E., Zrada, Matthew M., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, Abrams, Marc T., South, Vicki J., Huber, Hans E., Kohl, Nancy E., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
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Pyridyl aminothiazoles as potent Chk1 inhibitors: Optimization of cellular activity
Dudkin, Vadim Y., Wang, Cheng, Arrington, Kenneth L., Fraley, Mark E., Hartman, George D., Stirdivant, Steven M., Drakas, Robert A., Rickert, Keith, Walsh, Eileen S., Hamilton, Kelly, Buser, Carolyn A., Hardwick, James, Tao, Weikang, Beck, Stephen C., Mao, Xianzhi, Lobell, Robert B., Sepp-Lorenzino, Laura
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
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