未登录 A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors Liang, Rui; Tomita, Daisuke; Sasaki, Yusuke; Ginn, John; Michino, Mayako; Huggins, David J.; Baxt, Leigh; Kargman, Stacia; Shahid, Maaz; Aso, Kazuyoshi; Duggan, Mark; Stamford, Andrew W.; DeStanchina, Elisa; Liverton, Nigel; Meinke, Peter T.; Foley, Michael A.; Phillips, Richard E. 分享 收藏
Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules Singh, Kamini; Lin, Jianan; Lecomte, Nicolas; Mohan, Prathibha; Gokce, Askan; Sanghvi, Viraj R.; Jiang, Man; Grbovic-Huezo, Olivera; Burcul, Antonija; Stark, Stefan G.; Romesser, Paul B.; Chang, Qing; Melchor, Jerry P.; Beyer, Rachel K.; Duggan, Mark; Fukase, Yoshiyuki; Yang, Guangli; Ouerfelli, Ouathek; Viale, Agnes; de Stanchina, Elisa; Stamford, Andrew W.; Meinke, Peter T.; Raetsch, Gunnar; Leach, Steven D.; Ouyang, Zhengqing; Wendel, Hans-Guido 分享 收藏
Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity Johansson, Patrik; Kaspersson, Karin; Gurrell, Ian K.; Back, Elisabeth; Eketjall, Susanna; Scott, Clay W.; Cebers, Gvido; Thorne, Philip; McKenzie, Michael J.; Beaton, Haydn; Davey, Paul; Kolmodin, Karin; Holenz, Jorg; Duggan, Mark E.; Haeberlein, Samantha Budd; Burli, Roland W. 分享 收藏
The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity Cardarelli, Ross A.; Jones, Karen; Pisella, Lucie I.; Wobst, Heike J.; McWilliams, Lisa J.; Sharpe, Paul M.; Burnham, Matthew P.; Baker, David J.; Chudotvorova, Ilona; Guyot, Justine; Silayeva, Liliya; Morrow, Danielle H.; Dekker, Niek; Zicha, Stephen; Davies, Paul A.; Holenz, Jorg; Duggan, Mark E.; Dunlop, John; Mather, Robert J.; Wang, Qi; Medina, Igor; Brandon, Nicholas J.; Deeb, Tarek Z.; Moss, Stephen J. 分享 收藏
Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia Wood, Michael R.; Noetzel, Meredith J.; Melancon, Bruce J.; Poslusney, Michael S.; Nance, Kellie D.; Hurtado, Miguel A.; Luscombe, Vincent B.; Weiner, Rebecca L.; Rodriguez, Alice L.; Lamsal, Atin; Chang, Sichen; Bubser, Michael; Blobaum, Anna L.; Engers, Darren W.; Niswender, Colleen M.; Jones, Carrie K.; Brandon, Nicholas J.; Wood, Michael W.; Duggan, Mark E.; Conn, P. Jeffrey; Bridges, Thomas M.; Lindsley, Craig W. 分享 收藏
Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents M4毒蕈碱型乙酰胆碱受体的选择性激活可逆转MK-801-Induced行为障碍并增强啮齿动物的联想学习 Bubser, Michael; Bridges, Thomas M.; Dencker, Ditte; Gould, Robert W.; Grannan, Michael; Noetzel, Meredith J.; Lamsal, Atin; Niswender, Colleen M.; Daniels, J. Scott; Poslusney, Michael S.; Melancon, Bruce J.; Tarr, James C.; Byers, Frank W.; Wess, Juergen; Duggan, Mark E.; Dunlop, John; Wood, Michael W.; Brandon, Nicholas J.; Wood, Michael R.; Lindsley, Craig W.; Conn, P. Jeffrey; Jones, Carrie K. 分享 收藏
Discovery of the Selective Androgen Receptor Modulator MK-0773 Using a Rational Development Strategy Based on Differential Transcriptional Requirements for Androgenic Anabolism Versus Reproductive Physiology Schmidt, Azriel; Kimmel, Donald B.; Bai, Chang; Scafonas, Angela; Rutledge, SuJane; Vogel, Robert L.; McElwee-Witmer, Sheila; Chen, Fang; Nantermet, Pascale V.; Kasparcova, Viera; Leu, Chih-tai; Zhang, Hai-Zhuan; Duggan, Mark E.; Gentile, Michael A.; Hodor, Paul; Pennypacker, Brenda; Masarachia, Patricia; Opas, Evan E.; Adamski, Sharon A.; Cusick, Tara E.; Wang, Jiabing; Mitchell, Helen J.; Kim, Yuntae; Prueksaritanont, Thomayant; Perkins, James J.; Meissner, Robert S.; Hartman, George D.; Freedman, Leonard P.; Harada, Shun-ichi; Ray, William J. 分享 收藏
Identification of Anabolic Selective Androgen Receptor Modulators with Reduced Activities in Reproductive Tissues and Sebaceous Glands Schmidt, Azriel; Harada, Shun-Ichi; Kimmel, Donald B.; Bai, Chang; Chen, Fang; Rutledge, Su Jane; Vogel, Robert L.; Scafonas, Angela; Gentile, Michael A.; Nantermet, Pascale V.; McElwee-Witmer, Sheila; Pennypacker, Brenda; Masarachia, Patricia; Sahoo, Soumya P.; Kim, Yuntae; Meissner, Robert S.; Hartman, George D.; Duggan, Mark E.; Rodan, Gideon A.; Towler, Dwight A.; Ray, William J. 分享 收藏
Design, Synthesis, and Biological Evaluation 16-Substituted 4-Azasteroids as Tissue-Selective Androgen Receptor Modulators (SARMs) Mitchell, Helen J.; Dankulich, William P.; Hartman, George D.; Prueksaritanont, Thomayant; Schmidt, Azriel; Vogel, Robert L.; Bai, Chang; McElwee-Witmer, Sheila; Zhang, Hai Z.; Chen, Fang; Leu, Chih-Tai; Kimmel, Donald B.; Ray, William J.; Nantermet, Pascale; Gentile, Michael A.; Duggan, Mark E.; Meissner, Robert S. 分享 收藏
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Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1(propylsulfonyl)piperidin-4-yl]lmethyl benzamides Lindsley, Craig W.; Zhao, Zhijian; Leister, William H.; O'Brien, Julie; Lemaire, Wei; Williams, David L., Jr.; Chen, Tsing-Bau; Chang, Raymond S. L.; Burno, Maryann; Jacobson, Marlene A.; Sur, Cyrille; Kinney, Gene G.; Pettibone, Douglas J.; Tiller, Philip R.; Smith, Sheri; Tsou, Nancy N.; Duggan, Mark E.; Conn, P. Jeffrey; Hartman, George D. 分享 收藏
Difference in mGluR5 interaction between positive allosteric modulators from two structural classes 来自两个结构课程的正变构调节剂之间mGluR5相互作用的差异 Williams, DL; O'Brien, JA; Lemaire, W; Chen, TB; Chang, RSL; Jacobson, MA; Ha, SN; Wisnoski, DD; Lindsley, CW; Sur, C; Duggan, ME; Pettibone, DJ; Conn, PJ 分享 收藏
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models Kinney, GG; O'Brien, JA; Lemaire, W; Burno, M; Bickel, DJ; Clements, MK; Chen, TB; Wisnoski, DD; Lindsley, CW; Tiller, PR; Smith, S; Jacobson, MA; Sur, C; Duggan, ME; Pettibone, DJ; Conn, PJ; Williams, DL 分享 收藏
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Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides that potentiate receptor function in vivo Lindsley, CW; Wisnoski, DD; Leister, WH; O'Brien, JA; Lemaire, W; Williams, DL; Burno, M; Sur, C; Kinney, GG; Pettibone, DJ; Tiller, PR; Smith, S; Duggan, M; Hartman, GD; Conn, PJ; Huff, JR 分享 收藏
Nonpeptide αvβ3 antagonists.: Part 11:: Discovery and preclinical evaluation of potent αvβ3 antagonists for the prevention and treatment of osteoporosis Coleman, PJ; Brashear, KM; Askew, BC; Hutchinson, JH; McVean, CA; Duong, LT; Feuston, BP; Fernandez-Metzler, C; Gentile, MA; Hartman, GD; Kimmel, DB; Leu, CT; Lipfert, L; Merkle, K; Pennypacker, B; Prueksaritanont, T; Rodan, GA; Wesolowski, GA; Rodan, SB; Duggan, ME 分享 收藏
A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain O'Brien, JA; Lemaire, W; Wittmann, M; Jacobson, MA; Ha, SN; Wisnoski, DD; Lindsley, CW; Schaffhauser, HJ; Rowe, B; Sur, C; Duggan, ME; Pettibone, DJ; Conn, PJ; Williams, DL 分享 收藏
Nonpeptide αvβ3 antagonists.: 8.: In vitro and in vivo evaluation of a potent αvβ3 antagonist for the prevention and treatment of osteoporosis Hutchinson, JH; Hatczenko, W; Brashear, KM; Breslin, MJ; Coleman, PJ; Duong, LT; Fernandez-Metzler, C; Gentile, MA; Fisher, JE; Hartman, GD; Huff, JR; Kimmel, DB; Leu, CT; Meissner, RS; Merkle, K; Nagy, R; Pennypacker, B; Perkins, JJ; Prueksaritanont, T; Rodan, GA; Varga, SL; Wesolowski, GA; Zartman, AE; Rodan, SB; Duggan, ME 分享 收藏
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