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1
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Discovery of N-{N-(3-cyanophenyl)sulfonyl-4(R)-cyclobutylamino-(L)-prolyl}-4-(3',5'-dichloroisonicotinoyl) amino-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4

Lin, Linus S ; Lanza, Thomas ; Jewell, James P ; Liu, Ping ; Jones, Carrie ; Kieczykowski, Gerard R ; Treonze, Kelly ; Si, Qian ; Manior, Salony ; Koo, Gloria ; Tong, Xinchun ; Wang, Junying ; Schuelke, Anne ; Pivnichny, James ; Wang, Regina ; Raab, Conrad ; Vincent, Stella ; Davies, Philip ; Maccoss, Malcolm ; Mumford

Journal of medicinal chemistry, 11 June 2009, Vol.52(11), pp.3449-52 [Peer Reviewed Journal]

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2
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A facile microwave-assisted palladium-catalyzed cyanation of aryl chlorides

Chobanian, Harry R ; Fors, Brett P ; Lin, Linus S

Tetrahedron Letters, 2006, Vol.47(19), pp.3303-3305 [Peer Reviewed Journal]

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3
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Enantioselective approach to 3-substituted prolines

Kamenecka, Theodore M ; Park, You-Jung ; Lin, Linus S ; Lanza, Thomas ; Hagmann, William K

Tetrahedron Letters, 2001, Vol.42(49), pp.8571-8573 [Peer Reviewed Journal]

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4
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The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Lanza, Thomas J ; Chioda, Marc ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Raustad, Katie ; Wang, Sheng-Ping ; Strack, Alison M ; Gorski, Judith N ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic

Bioorganic & medicinal chemistry, 01 May 2012, Vol.20(9), pp.2845-9 [Peer Reviewed Journal]

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5
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A facile, microwave-assisted, palladium-catalyzed arylation of acetone

Chobanian, Harry R ; Liu, Ping ; Chioda, Marc D ; Guo, Yan ; Lin, Linus S

Tetrahedron Letters, 2007, Vol.48(7), pp.1213-1216 [Peer Reviewed Journal]

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6
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A highly active catalyst system for the heteroarylation of acetone

Liu, Ping ; Lanza, Thomas J ; Jewell, James P ; Jones, Carrie P ; Hagmann, William K ; Lin, Linus S

Tetrahedron Letters, 2003, Vol.44(49), pp.8869-8871 [Peer Reviewed Journal]

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7
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Similar in vitro pharmacology of human cannabinoid CB 1 receptor variants expressed in CHO cells

Xiao, Jing Chen ; Jewell, James P ; Lin, Linus S ; Hagmann, William K ; Fong, Tung M ; Shen, Chun-Pyn

Brain Research, 2008, Vol.1238, pp.36-43 [Peer Reviewed Journal]

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8
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Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists

Lo, Michael M.-C ; Chobanian, Harry R ; Palyha, Oksana ; Kan, Yanqing ; Kelly, Theresa M ; Guan, Xiao-Ming ; Reitman, Marc L ; Dragovic, Jasminka ; Lyons, Kathryn A ; Nargund, Ravi P ; Lin, Linus S

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(7), pp.2040-2043 [Peer Reviewed Journal]

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9
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Deprotection of N- tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters

Lin, Linus S ; Lanza, Thomas ; de Laszlo, Stephen E ; Truong, Quang ; Kamenecka, Theodore ; Hagmann, William K

Tetrahedron Letters, 2000, Vol.41(36), pp.7013-7016 [Peer Reviewed Journal]

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10
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Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase

Liu, Ping ; Hamill, Terence G ; Chioda, Marc ; Chobanian, Harry ; Fung, Selena ; Guo, Yan ; Chang, Linda ; Bakshi, Raman ; Hong, Qingmei ; Dellureficio, James ; Lin, Linus S ; Abbadie, Catherine ; Alexander, Jessica ; Jin, Hong ; Mandala, Suzanne ; Shiao, Lin-Lin ; Li, Wenping ; Sanabria, Sandra ; Williams, David ; Zeng

ACS medicinal chemistry letters, 13 June 2013, Vol.4(6), pp.509-13 [Peer Reviewed Journal]

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11
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Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3 H-pyrazolo[3,4- c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists

Guo, Cheng ; Guzzo, Peter R ; Hadden, Mark ; Sargent, Bruce J ; Yet, Larry ; Kan, Yanqing ; Palyha, Oksana ; Kelly, Theresa M ; Guan, Xiaoming ; Rosko, Kim ; Gagen, Karen ; Metzger, Joseph M ; Dragovic, Jasminka ; Lyons, Kathryn ; Lin, Linus S ; Nargund, Ravi P

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(9), pp.2785-2789 [Peer Reviewed Journal]

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12
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Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant

Kopka, Ihor E ; Lin, Linus S ; Jewell, James P ; Lanza, Thomas J ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Zhege J ; Ha, Sookhee ; Castonguay, Laurie G ; Van Der Ploeg, Lex ; Goulet, Mark T ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(16), pp.4757-4761 [Peer Reviewed Journal]

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13
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Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments

Metzger, Joseph M ; Gagen, Karen ; Raustad, Kate A ; Yang, Liming ; White, Amanda ; Wang, Sheng-Ping ; Craw, Stephanie ; Liu, Ping ; Lanza, Thomas ; Lin, Linus S ; Nargund, Ravi P ; Guan, Xiao-Ming ; Strack, Alison M ; Reitman, Marc L

American journal of physiology. Endocrinology and metabolism, November 2010, Vol.299(5), pp.E816-24 [Peer Reviewed Journal]

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14
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Conformational analysis and receptor docking of N-(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl-2-methyl-2-{5-(trifluoromethyl)pyridin-2-yloxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist

Lin, Linus S ; Ha, Sookhee ; Ball, Richard G ; Tsou, Nancy N ; Castonguay, Laurie A ; Doss, George A ; Fong, Tung M ; Shen, Chun-Pyn ; Xiao, Jing Chen ; Goulet, Mark T ; Hagmann, William K

Journal of medicinal chemistry, 10 April 2008, Vol.51(7), pp.2108-14 [Peer Reviewed Journal]

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15
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Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Chioda, Marc ; Lanza, Thomas J ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Gorski, Judith N ; Raustad, Kate ; Wang, Sheng-Ping ; Strack, Alison M ; Miller, Randy ; Pang, Jianmei ; Madeira, Maria ; Lyons

ACS medicinal chemistry letters, 08 March 2012, Vol.3(3), pp.252-6 [Peer Reviewed Journal]

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16
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Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist

Guan, Xiao-Ming ; Metzger, Joseph M ; Yang, Liming ; Raustad, Kate A ; Wang, Sheng-Ping ; Spann, Stephanie K ; Kosinski, Jennifer A ; Yu, Hong ; Shearman, Lauren P ; Faidley, Terry D ; Palyha, Oksana ; Kan, Yanqing ; Kelly, Theresa M ; Sebhat, Iyassu ; Lin, Linus S ; Dragovic, Jasminka ; Lyons, Kathy A ; Craw, Stephanie ; Nargund, Ravi P ; Marsh

The Journal of pharmacology and experimental therapeutics, February 2011, Vol.336(2), pp.356-64 [Peer Reviewed Journal]

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17
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Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

Sebhat, Iyassu K ; Franklin, Christopher ; Lo, Michael M-C ; Chen, David ; Jewell, James P ; Miller, Randy ; Pang, Jianmei ; Palyha, Oksana ; Kan, Yanqing ; Kelly, Theresa M ; Guan, Xiao-Ming ; Marsh, Donald J ; Kosinski, Jennifer A ; Metzger, Joseph M ; Lyons, Kathryn ; Dragovic, Jasminka ; Guzzo, Peter R ; Henderson, Alan J ; Reitman, Marc L ; Nargund

ACS medicinal chemistry letters, 13 January 2011, Vol.2(1), pp.43-7 [Peer Reviewed Journal]

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18
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Effects of mutations at conserved TM II residues on ligand binding and activation of mouse 5-HT 6 receptor

Zhang, Jiaping ; Shen, Chun-Pyn ; Xiao, Jing C ; Lanza, Thomas J ; Lin, Linus S ; Francis, Barbara E ; Fong, Tung M ; Chen, Richard Z

European Journal of Pharmacology, 2006, Vol.534(1), pp.77-82 [Peer Reviewed Journal]

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19
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Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity

Hadden, Mark ; Goodman, Allan ; Guo, Cheng ; Guzzo, Peter R ; Henderson, Alan J ; Pattamana, Kevin ; Ruenz, Megan ; Sargent, Bruce J ; Swenson, Brian ; Yet, Larry ; Liu, Jian ; He, Shuwen ; Sebhat, Iyassu K ; Lin, Linus S ; Tamvakopoulos, Constantin ; Peng, Qianping ; Kan, Yanqing ; Palyha, Oksana ; Kelly, Theresa M ; Guan, Xiao-Ming

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(9), pp.2912-2915 [Peer Reviewed Journal]

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20
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Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity

Liu, Jian ; He, Shuwen ; Jian, Tianying ; Dobbelaar, Peter H ; Sebhat, Iyassu K ; Lin, Linus S ; Goodman, Allan ; Guo, Cheng ; Guzzo, Peter R ; Hadden, Mark ; Henderson, Alan J ; Pattamana, Kevin ; Ruenz, Megan ; Sargent, Bruce J ; Swenson, Brian ; Yet, Larry ; Tamvakopoulos, Constantin ; Peng, Qianping ; Pan, Jie ; Kan, Yanqing

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(7), pp.2074-2077 [Peer Reviewed Journal]

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21
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Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-4-(2-18Ffluoroethoxy)phenyl-1-methylpropyl}- 2-methyl-2-(5-methylpyridin-2-yl)oxypropanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use

Liu, Ping ; Lin, Linus S ; Hamill, Terence G ; Jewell, James P ; Lanza, Thomas J ; Gibson, Raymond E ; Krause, Stephen M ; Ryan, Christine ; Eng, Waisi ; Sanabria, Sandra ; Tong, Xinchun ; Wang, Junying ; Levorse, Dorothy A ; Owens, Karen A ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Kumar, Sanjeev ; Yin, Wenji ; Payack

Journal of medicinal chemistry, 26 July 2007, Vol.50(15), pp.3427-30 [Peer Reviewed Journal]

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22
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Discovery of N-(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl-2-methyl-2- {5-(trifluoromethyl)pyridin-2-yloxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity

Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Liu, Ping ; Shah, Shrenik K ; Qi, Hongbo ; Tong, Xinchun ; Wang, Junying ; Xu, Suoyu S ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Xiao, Jing Chen ; Shearman, Lauren P ; Stribling, D Sloan ; Rosko, Kimberly ; Strack, Alison ; Marsh, Donald J ; Feng, Yue ; Kumar

Journal of medicinal chemistry, 28 December 2006, Vol.49(26), pp.7584-7 [Peer Reviewed Journal]

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23
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18FMK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor

Burns, H Donald ; Van Laere, Koen ; Sanabria-Bohórquez, Sandra ; Hamill, Terence G ; Bormans, Guy ; Eng, Wai-Si ; Gibson, Ray ; Ryan, Christine ; Connolly, Brett ; Patel, Shil ; Krause, Stephen ; Vanko, Amy ; Van Hecken, Anne ; Dupont, Patrick ; De Lepeleire, Inge ; Rothenberg, Paul ; Stoch, S Aubrey ; Cote, Josee ; Hagmann

Proceedings of the National Academy of Sciences of the United States of America, 05 June 2007, Vol.104(23), pp.9800-5 [Peer Reviewed Journal]

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24
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[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor

Burns, H Donald ; Van Laere, Koen ; Sanabria-Bohórquez, Sandra ; Hamill, Terence G ; Bormans, Guy ; Eng, Wai-si ; Gibson, Ray ; Ryan, Christine ; Connolly, Brett ; Patel, Shil ; Krause, Stephen ; Vanko, Amy ; Van Hecken, Anne ; Dupont, Patrick ; De Lepeleire, Inge ; Rothenberg, Paul ; Stoch, S Aubrey ; Cote, Josee ; Hagmann, William K ; Jewell, James P ; Lin, Linus S ; Liu, Ping ; Goulet, Mark T ; Gottesdiener, Keith ; Wagner, John A ; de Hoon, Jan ; Mortelmans, Luc ; Fong, Tung M ; Hargreaves, Richard J

Proceedings of the National Academy of Sciences of the United States of America, 2007-06, Vol.104(23), pp.9800-9805 [Peer Reviewed Journal]

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25
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Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality

Liu, Ping ; Lanza, Thomas J ; Chioda, Marc ; Jones, Carrie ; Chobanian, Harry R ; Guo, Yan ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Ramsay, Katie ; Wang, Sheng-Ping ; Strack, Alison M ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic

ACS medicinal chemistry letters, 08 December 2011, Vol.2(12), pp.933-7 [Peer Reviewed Journal]

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26
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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Chioda, Marc D ; Fung, Selena ; Lanza, Thomas J ; Chang, Linda ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Mclaughlin, Mark ; Belyk, Kevin M ; Krska, Shane W ; Makarewicz, Amanda K ; Martel, Elliot J ; Leone, Joseph F ; Frey, Lisa ; Karanam, Bindhu ; Madeira, Maria ; Alvaro

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.717-21 [Peer Reviewed Journal]

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27
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Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists

He, Shuwen ; Dobbelaar, Peter H ; Liu, Jian ; Jian, Tianying ; Sebhat, Iyassu K ; Lin, Linus S ; Goodman, Allan ; Guo, Cheng ; Guzzo, Peter R ; Hadden, Mark ; Henderson, Alan J ; Ruenz, Megan ; Sargent, Bruce J ; Yet, Larry ; Kelly, Theresa M ; Palyha, Oksana ; Kan, Yanqing ; Pan, Jie ; Chen, Howard ; Marsh, Donald J

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(6), pp.1913-1917 [Peer Reviewed Journal]

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28
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Synthesis of [3,5‐dichlorobenzenesulfonamide‐U‐ 14 C)] labeled VLA‐4 antagonists

Yu, Nathan X. ; Raab, Conrad E. ; Dean, Dennis C. ; Lin, Linus S. ; Melillo, David G.

Journal of Labelled Compounds and Radiopharmaceuticals, February 2004, Vol.47(2), pp.115-125 [Peer Reviewed Journal]

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29
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Alpha(4)beta(7)/alpha(4)beta(1) dual integrin antagonists block alpha(4)beta(7)-dependent adhesion under shear flow

Egger, Linda A ; Kidambi, Usha ; Cao, Jin ; Van Riper, Gail ; Mccauley, Ermengilda ; Mumford, Richard A ; Amo, Suzanne ; Lingham, Russell ; Lanza, Thomas ; Lin, Linus S ; De Laszlo, Stephen E ; Young, David N ; Kopka, Ihor E ; Tong, Sharon ; Pikounis, Bill ; Benson, Evelyn ; Warwood, Sarah ; Bargatze, Robert F ; Hagmann, William K ; Schmidt

The Journal of pharmacology and experimental therapeutics, July 2002, Vol.302(1), pp.153-62 [Peer Reviewed Journal]

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30
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A small molecule alpha4beta1/alpha4beta7 antagonist differentiates between the low-affinity states of alpha4beta1 and alpha4beta7: characterization of divalent cation dependence

Egger, Linda A ; Cao, Jin ; Mccallum, Christine ; Kidambi, Usha ; Van Riper, Gail ; Mccauley, Ermengilda ; Mumford, Richard A ; Lanza, Thomas J ; Lin, Linus S ; De Laszlo, Stephen E ; Young, David N ; Yang, Ginger ; Dean, Dennis C ; Raab, Conrad E ; Wallace, Mike A ; Jones, Allen N ; Hagmann, William K ; Schmidt, John A ; Pepinsky, R Blake ; Scott

The Journal of pharmacology and experimental therapeutics, September 2003, Vol.306(3), pp.903-13 [Peer Reviewed Journal]

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31
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Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl-2-methyl-2-5-(trifluoromethyl)pyridin-2-yloxypropanamide (MK-0364), in rodents

Fong, Tung M ; Guan, Xiao-Ming ; Marsh, Donald J ; Shen, Chun-Pyn ; Stribling, D Sloan ; Rosko, Kim M ; Lao, Julie ; Yu, Hong ; Feng, Yue ; Xiao, Jing C ; Van Der Ploeg, Lex H T ; Goulet, Mark T ; Hagmann, Williams K ; Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Liu, Ping ; Shah, Shrenik K ; Qi, Hongbo ; Tong

The Journal of pharmacology and experimental therapeutics, June 2007, Vol.321(3), pp.1013-22 [Peer Reviewed Journal]

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32
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Synthesis and evaluation of N-[(1 S,2 S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists

Du, Wu ; Jewell, James P ; Lin, Linus S ; Colandrea, Vincent J ; Xiao, Jing C ; Lao, Julie ; Shen, Chun-Pyn ; Bateman, Thomas J ; Reddy, Vijay B.G ; Ha, Sookhee N ; Shah, Shrenik K ; Fong, Tung M ; Hale, Jeffrey J ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(17), pp.5195-5199 [Peer Reviewed Journal]

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33
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Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4

Lin, Linus S ; Lanza, Thomas J ; Castonguay, Laurie A ; Kamenecka, Theodore ; Mccauley, Ermenegilda ; Van Riper, Gail ; Egger, Linda A ; Mumford, Richard A ; Tong, Xinchun ; Maccoss, Malcolm ; Schmidt, John A ; Hagmann, William K

Bioorganic & medicinal chemistry letters, 03 May 2004, Vol.14(9), pp.2331-4 [Peer Reviewed Journal]

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34
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Specific and dual antagonists of α 4β 1 and α 4β 7 integrins

Lin, Linus S ; Lanza, Thomas ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Cao, Jin ; Egger, Linda A ; Mumford, Richard A ; Schmidt, John A ; Maccoss, Malcolm ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(2), pp.133-136 [Peer Reviewed Journal]

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35
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Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques

Samuel, Koppara ; Yin, Wenji ; Stearns, Ralph A. ; Tang, Yui S. ; Chaudhary, Ashok G. ; Jewell, James P. ; Lanza, Thomas ; Lin, Linus S. ; Hagmann, William K. ; Evans, David C. ; Kumar, Sanjeev

Journal of Mass Spectrometry, February 2003, Vol.38(2), pp.211-221 [Peer Reviewed Journal]

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36
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Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists

Armstrong, Helen E ; Galka, Amy ; Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Shah, Shrenik K ; Guthikonda, Ravi ; Truong, Quang ; Chang, Linda L ; Quaker, Grace ; Colandrea, Vincent J ; Tong, Xinchun ; Wang, Junying ; Xu, Sherry ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Chen, Jing ; Shearman, Lauren P ; Stribling, D. Sloan

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(8), pp.2184-2187 [Peer Reviewed Journal]

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