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2-(3aR,4R,5S,7aS)-5-{(1S)-1-3,5-bis(trifluoromethyl)phenyl-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways

Kassick, Andrew J ; Jiang, Jinlong ; Bunda, Jaime ; Wilson, David ; Bao, Jianming ; Lu, Huagang ; Lin, Peter ; Ball, Richard G ; Doss, George A ; Tong, Xinchun ; Tsao, Kwei-Lan C ; Wang, Hong ; Chicchi, Gary ; Karanam, Bindhu ; Tschirret-Guth, Richard ; Samuel, Koppara ; Hora, Donald F ; Kumar, Sanjeev ; Madeira, Maria ; Eng, Waisi ; Hargreaves, Richard ; Purcell, Mona ; Gantert, Liza ; Cook, Jacquelyn ; Devita, Robert J ; Mills, Sander G

Journal of medicinal chemistry, 25 July 2013, Vol.56(14), pp.5940-8 [Peer Reviewed Journal]

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Site-Specific, Enzymatic Biotinylation of Recombinant Proteins inSpodoptera frugiperdaCells Using Biotin Acceptor Peptides

Duffy, Siobain ; Tsao, Kwei-Lan ; Waugh, David S

Analytical Biochemistry, 10 September 1998, Vol.262(2), pp.122-128 [Peer Reviewed Journal]

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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists

Lai, Zhong ; He, Shuwen ; Sherer, Edward C ; Wu, Zhicai ; Yu, Yang ; Ball, Richard ; Hong, Qingmei ; Yang, David X ; Guo, Liangqing ; Li, Derun ; Tuang, Quang ; Chicchi, Gary G ; Trusca, Dorina ; Tsao, Kwei-Lan ; Zhou, Yun-Ping ; Howard, Andrew D ; Nargund, Ravi P ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 01 September 2015, Vol.25(17), pp.3520-3525 [Peer Reviewed Journal]

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Modulation of basal and stress‐induced amygdaloid substance P release by the potent and selective NK1 receptor antagonist L‐822429

Singewald, Nicolas ; Chicchi, Gary G. ; Thurner, Clemens C. ; Tsao, KweiLan ; Spetea, Mariana ; Schmidhammer, Helmut ; Sreepathi, Hari Kishore ; Ferraguti, Francesco ; Singewald, Georg M. ; Ebner, Karl

Journal of Neurochemistry, September 2008, Vol.106(6), pp.2476-2488 [Peer Reviewed Journal]

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Tetrahydroindolizinone NK 1 antagonists

Bao, Jianming ; Lu, Huagang ; Morriello, Gregori J ; Carlson, Emma J ; Wheeldon, Alan ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Zheng, Song ; Tong, Xinchun ; Mills, Sander G ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(7), pp.2354-2358 [Peer Reviewed Journal]

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Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition

Liu, Weiguo ; Shao, Pengcheng P ; Liang, Gui-Bai ; Bawiec, John ; He, Jiafang ; Aster, Susan D ; Wu, Margaret ; Chicchi, Garry ; Wang, John ; Tsao, Kwei-Lan ; Shang, Jin ; Salituro, Gino ; Zhou, Yun-Ping ; Li, Cai ; Akiyama, Taro E ; Metzger, Daniel E ; Murphy, Beth Ann ; Howard, Andrew D ; Weber, Ann E ; Duffy, Joseph L

ACS medicinal chemistry letters, 08 November 2018, Vol.9(11), pp.1082-1087 [Peer Reviewed Journal]

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Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist

Pasternak, Alexander ; Feng, Zhe ; De Jesus, Reynalda ; Ye, Zhixiong ; He, Shuwen ; Dobbelaar, Peter ; Bradley, Scott A ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Eiermann, George J ; Li, Cai ; Feng, Yue ; Wu, Margaret ; Shao, Qing ; Zhang, Bei B ; Nargund, Ravi ; Mills, Sander G ; Howard, Andrew D ; Yang, Lihu ; Zhou, Yun-Ping

ACS medicinal chemistry letters, 12 April 2012, Vol.3(4), pp.289-93 [Peer Reviewed Journal]

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Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists

Li, Derun ; Wu, Zhicai ; Yu, Yang ; Ball, Richard G ; Guo, Liangqin ; Sherer, Edward ; He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Qi, Hongbo ; Truong, Quang ; Yang, David X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Trujillo, Maria ; Pachanski, Michele ; Eiermann, George J ; Howard, Andrew D ; Zhou, Yun-Ping ; Zhang, Bei B ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.690-5 [Peer Reviewed Journal]

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Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists

Jiang, Jinlong ; Bunda, Jaime L ; Doss, Geoge A ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Tong, Xinchun ; Zheng, Song ; Upthagrove, Alana ; Samuel, Koppara ; Tschirret-Guth, Richard ; Kumar, Sanjeev ; Wheeldon, Alan ; Carlson, Emma J ; Hargreaves, Richard ; Burns, Donald ; Hamill, Terence ; Ryan, Christine ; Krause, Stephen M ; Eng, Waisi ; Devita, Robert J ; Mills, Sander G

Journal of medicinal chemistry, 14 May 2009, Vol.52(9), pp.3039-46 [Peer Reviewed Journal]

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Fused bicyclic pyrrolizinones as new scaffolds for human NK 1 antagonists

Morriello, Gregori J ; Devita, Robert J ; Mills, Sander G ; Young, Jonathan R ; Lin, Peter ; Doss, George ; Chicchi, Gary G ; Demartino, Julie ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Carlson, Emma ; Townson, Karen ; Wheeldon, Alan ; Boyce, Susan ; Collinson, Neil ; Rupniak, Nadia ; Moore, Stephen

Bioorganic & Medicinal Chemistry, 2008, Vol.16(5), pp.2156-2170 [Peer Reviewed Journal]

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Balancing the Production of Two Recombinant Proteins inEscherichia coliby Manipulating Plasmid Copy Number: High-Level Expression of Heterodimeric Ras Farnesyltransferase

Tsao, Kwei-Lan ; Waugh, David S

Protein Expression and Purification, December 1997, Vol.11(3), pp.233-240 [Peer Reviewed Journal]

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12
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Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists

He, Shuwen ; Lai, Zhong ; Ye, Zhixiong ; Dobbelaar, Peter H ; Shah, Shrenik K ; Truong, Quang ; Du, Wu ; Guo, Liangqin ; Liu, Jian ; Jian, Tianying ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James ; Reibarkh, Mikhail ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Kerr, Janet ; Fitzgerald, Patrick ; Morissette, Pierre ; Volksdorf, Sylvia ; Eiermann, George J ; Li, Cai ; Zhang, Bei ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 10 July 2014, Vol.5(7), pp.748-53 [Peer Reviewed Journal]

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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists

He, Shuwen ; Dobbelaar, Peter H ; Guo, Liangqin ; Ye, Zhixiong ; Liu, Jian ; Jian, Tianying ; Truong, Quang ; Shah, Shrenik K ; Du, Wu ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James D ; Sherer, Edward ; Pasternak, Alexander ; Feng, Zhe ; Reibarkh, Mikhail ; Lin, Melissa ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Kerr, Janet ; Fitzgerald, Patrick ; Morissette, Pierre ; Volksdorf, Sylvia ; Eiermann, George J ; Li, Cai ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 15 March 2016, Vol.26(6), pp.1529-1535 [Peer Reviewed Journal]

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14
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Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

Shah, Shrenik K ; He, Shuwen ; Guo, Liangqin ; Truong, Quang ; Qi, Hongbo ; Du, Wu ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Hong, Qingmei ; Dobbelaar, Peter ; Ye, Zhixiong ; Sherer, Edward ; Feng, Zhe ; Yu, Yang ; Wong, Frederick ; Samuel, Koppara ; Madiera, Maria ; Karanam, Bindhu V ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Feng, Yue ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Eiermann, George J ; Li, Cai ; Pachanski, Michele ; Fernandez, Guillermo ; Nelson, Donald ; Bunting, Patricia ; Morissette, Pierre ; Volksdorf, Sylvia ; Kerr, Janet ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Pasternak, Alexander ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 14 May 2015, Vol.6(5), pp.513-7 [Peer Reviewed Journal]

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15
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The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes

He, Shuwen ; Ye, Zhixiong ; Truong, Quang ; Shah, Shrenik ; Du, Wu ; Guo, Liangqin ; Dobbelaar, Peter H ; Lai, Zhong ; Liu, Jian ; Jian, Tianying ; Qi, Hongbo ; Bakshi, Raman K ; Hong, Qingmei ; Dellureficio, James ; Pasternak, Alexander ; Feng, Zhe ; Dejesus, Reynalda ; Yang, Lihu ; Reibarkh, Mikhail ; Bradley, Scott A ; Holmes, Mark A ; Ball, Richard G ; Ruck, Rebecca T ; Huffman, Mark A ; Wong, Frederick ; Samuel, Koppara ; Reddy, Vijay B ; Mitelman, Stan ; Tong, Sharon X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Wu, Margaret ; Shao, Qing ; Trujillo, Maria E ; Eiermann, George J ; Li, Cai ; Zhang, Bei B ; Howard, Andrew D ; Zhou, Yun-Ping ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 14 June 2012, Vol.3(6), pp.484-9 [Peer Reviewed Journal]

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16
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A versatile plasmid expression vector for the production of biotinylated proteins by site-specific, enzymatic modification in Escherichia coli

Tsao, Kwei-Lan ; Debarbieri, Barbara ; Michel, Hanspeter ; Waugh, David S

Gene, 1996, Vol.169(1), pp.59-64 [Peer Reviewed Journal]

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17
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Synthesis and structure–activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK 1 antagonists

Thomson, Christopher G ; Carlson, Emma ; Chicchi, Gary G ; Kulagowski, Janusz J ; Kurtz, Marc M ; Swain, Christopher J ; Tsao, Kwei-Lan C ; Wheeldon, Alan

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(4), pp.811-814 [Peer Reviewed Journal]

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18
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Pyrrolidine-carboxamides and oxadiazoles as potent hNK 1 antagonists

Young, Jonathan R ; Eid, Ronsar ; Turner, Cherilyn ; Devita, Robert J ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Chicchi, Gary G ; Wheeldon, Alan ; Carlson, Emma ; Mills, Sander G

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(19), pp.5310-5315 [Peer Reviewed Journal]

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19
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NK 1 antagonists based on seven membered lactam scaffolds

Elliott, Jason M ; Carlson, Emma J ; Chicchi, Gary G ; Dirat, Olivier ; Dominguez, Maria ; Gerhard, Ute ; Jelley, Richard ; Jones, A. Brian ; Kurtz, Marc M ; Tsao, Kwei Lan ; Wheeldon, Alan

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(11), pp.2929-2932 [Peer Reviewed Journal]

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20
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Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR

Finke, Paul E ; Meurer, Laura C ; Levorse, Dorothy A ; Mills, Sander G ; Maccoss, Malcolm ; Sadowski, Sharon ; Cascieri, Margaret A ; Tsao, Kwei-Lan ; Chicchi, Gary G ; Metzger, Joseph M ; Macintyre, D. Euan

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4497-4503 [Peer Reviewed Journal]

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21
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2-Aryl indole NK 1 receptor antagonists: optimisation of the 2-Aryl ring and the indole nitrogen substituent

Dinnell, Kevin ; Chicchi, Gary G ; Dhar, Madhumeeta J ; Elliott, Jason M ; Hollingworth, Gregory J ; Kurtz, Marc M ; Ridgill, Mark P ; Rycroft, Wayne ; Tsao, Kwei-Lan ; Williams, Angela R ; Swain, Christopher J

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(9), pp.1237-1240 [Peer Reviewed Journal]

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22
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The discovery of potent, selective, and orally bioavailable hNK 1 antagonists derived from pyrrolidine

Lin, Peter ; Chang, Lehua ; Devita, Robert J ; Young, Jonathan R ; Eid, Ronsar ; Tong, Xinchun ; Zheng, Song ; Ball, Richard G ; Tsou, Nancy N ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Wheeldon, Alan ; Carlson, Emma J ; Eng, Waisi ; Burns, H. Donald ; Hargreaves, Richard J ; Mills, Sander G

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(18), pp.5191-5198 [Peer Reviewed Journal]

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23
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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Elliott, Jason M ; Carling, Robert W ; Chambers, Mark ; Chicchi, Gary G ; Hutson, Peter H ; Jones, A Brian ; Macleod, Angus ; Marwood, Rose ; Meneses-Lorente, Georgina ; Mezzogori, Elena ; Murray, Fraser ; Rigby, Michael ; Royo, Inmaculada ; Russell, Michael G N ; Sohal, Bindi ; Tsao, Kwei Lan ; Williams, Brian

Bioorganic & medicinal chemistry letters, 15 November 2006, Vol.16(22), pp.5748-51 [Peer Reviewed Journal]

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24
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N′,2-Diphenylquinoline-4-carbohydrazide based NK 3 receptor antagonists II

Elliott, Jason M ; Carling, Robert W ; Chicchi, Gary G ; Crawforth, James ; Hutson, Peter H ; Jones, A. Brian ; Kelly, Sarah ; Marwood, Rose ; Meneses-Lorente, Georgina ; Mezzogori, Elena ; Murray, Fraser ; Rigby, Michael ; Royo, Inmaculada ; Russell, Michael G.N ; Shaw, Duncan ; Sohal, Bindi ; Tsao, Kwei Lan ; Williams, Brian

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(22), pp.5752-5756 [Peer Reviewed Journal]

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25
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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II

Elliott, Jason M ; Carling, Robert W ; Chicchi, Gary G ; Crawforth, James ; Hutson, Peter H ; Jones, A Brian ; Kelly, Sarah ; Marwood, Rose ; Meneses-Lorente, Georgina ; Mezzogori, Elena ; Murray, Fraser ; Rigby, Michael ; Royo, Inmaculada ; Russell, Michael G N ; Shaw, Duncan ; Sohal, Bindi ; Tsao, Kwei Lan ; Williams, Brian

Bioorganic & medicinal chemistry letters, 15 November 2006, Vol.16(22), pp.5752-6 [Peer Reviewed Journal]

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26
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Novel lactam NK 1 antagonists with anti-emetic activity

Hollingworth, Gregory J ; Carlson, Emma J ; Castro, José L ; Chicchi, Gary G ; Clark, Natalie ; Cooper, Laura C ; Dirat, Olivier ; Salvo, Jerry Di ; Elliott, Jason M ; Kilburn, Ruth ; Kurtz, Marc M ; Rycroft, Wayne ; Tattersall, F. David ; Tsao, Kwei-Lan ; Swain, Christopher J

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(5), pp.1197-1201 [Peer Reviewed Journal]

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27
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N′,2-Diphenylquinoline-4-carbohydrazide based NK 3 receptor antagonists

Elliott, Jason M ; Carling, Robert W ; Chambers, Mark ; Chicchi, Gary G ; Hutson, Peter H ; Jones, A. Brian ; Macleod, Angus ; Marwood, Rose ; Meneses-Lorente, Georgina ; Mezzogori, Elena ; Murray, Fraser ; Rigby, Michael ; Royo, Inmaculada ; Russell, Michael G.N ; Sohal, Bindi ; Tsao, Kwei Lan ; Williams, Brian

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(22), pp.5748-5751 [Peer Reviewed Journal]

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28
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4,4-Disubstituted cyclohexylamine NK 1 receptor antagonists I

Elliott, Jason M ; Castro, Jose L ; Chicchi, Gary G ; Cooper, Laura C ; Dinnell, Kevin ; Hollingworth, Gregory J ; Ridgill, Mark P ; Rycroft, Wayne ; Kurtz, Marc M ; Shaw, Duncan E ; Swain, Christopher J ; Tsao, Kwei-Lan ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(13), pp.1755-1758 [Peer Reviewed Journal]

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29
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2-Aryl Indole NK 1 receptor antagonists: optimisation of indole substitution

Cooper, Laura C ; Chicchi, Gary G ; Dinnell, Kevin ; Elliott, Jason M ; Hollingworth, Gregory J ; Kurtz, Marc M ; Locker, Karen L ; Morrison, Denise ; Shaw, Duncan E ; Tsao, Kwei-Lan ; Watt, Alan P ; Williams, Angela R ; Swain, Christopher J

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(9), pp.1233-1236 [Peer Reviewed Journal]

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30
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4,4-Disubstituted cyclohexylamine NK 1 receptor antagonists II

Cooper, Laura C ; Carlson, Emma J ; Castro, Jose L ; Chicchi, Gary G ; Dinnell, Kevin ; Di Salvo, Jerry ; Elliott, Jason M ; Hollingworth, Gregory J ; Kurtz, Marc M ; Ridgill, Mark P ; Rycroft, Wayne ; Tsao, Kwei-Lan ; Swain, Christopher J

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(13), pp.1759-1762 [Peer Reviewed Journal]

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31
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Comparison of the functional blockade of rat substance P (NK 1) receptors by GR205171, RP67580, SR140333 and NKP-608

Rupniak, Nadia M.J ; Carlson, Emma J ; Shepheard, Sara ; Bentley, Graham ; Williams, Angela R ; Hill, Alastair ; Swain, Christopher ; Mills, Sander G ; Di Salvo, Jerry ; Kilburn, Ruth ; Cascieri, Margaret A ; Kurtz, Marc M ; Tsao, Kwei-Lan ; Gould, Sandra L ; Chicchi, Gary G

Neuropharmacology, 2003, Vol.45(2), pp.231-241 [Peer Reviewed Journal]

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32
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Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

Meurer, Laura C ; Finke, Paul E ; Owens, Karen A ; Tsou, Nancy N ; Ball, Richard G ; Mills, Sander G ; Maccoss, Malcolm ; Sadowski, Sharon ; Cascieri, Margaret A ; Tsao, Kwei-Lan ; Chicchi, Gary G ; Egger, Linda A ; Luell, Silvi ; Metzger, Joseph M ; Macintyre, D. Euan ; Rupniak, Nadia M.J ; Williams, Angela R ; Hargreaves, Richard J

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4504-4511 [Peer Reviewed Journal]

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33
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CCDC 603506: Experimental Crystal Structure Determination

Meurer, L.C. ; Finke, P.E. ; Owens, K.A. ; Tsou, N.N. ; Ball, R.G. ; Mills, S.G. ; MacCoss, M. ; Sadowski, S. ; Cascieri, M.A. ; Tsao, Kwei-Lan ; Chicchi, G.G. ; Egger, L.A. ; Luell, S. ; Metzger, J.M. ; MacIntyre, D.E. ; Rupniak, N.M.J. ; Williams, A.R. ; Hargreaves, R.J.

2007

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