Integrating the Impact of Lipophilicity on Potency and Pharmacokinetic Parameters Enables the Use of Diverse Chemical Space during Small Molecule Drug Optimization von Miller, Randy R, Madeira, Maria, Wood, Harold B, Geissler, Wayne M, Raab, Conrad E, Martin, Iain J

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GPR119 Agonism Increases Glucagon Secretion During Insulin-Induced Hypoglycemia von Li, Nina Xiaoyan, Brown, Stacey, Kowalski, Tim, Wu, Margaret, Yang, Liming, Dai, Ge, Petrov, Aleksandr, Ding, Yuyan, Dlugos, Tamara, Wood, Harold B, Wang, Liangsu, Erion, Mark, Sherwin, Robert, Kelley, David E

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A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors von Tucker, Thomas J, Embrey, Mark W, Alleyne, Candice, Amin, Rupesh P, Bass, Alan, Bhatt, Bhavana, Bianchi, Elisabetta, Branca, Danila, Bueters, Tjerk, Buist, Nicole, Ha, Sookhee N, Hafey, Mike, He, Huaibing, Higgins, John, Johns, Douglas G, Kerekes, Angela D, Koeplinger, Kenneth A, Kuethe, Jeffrey T, Li, Nianyu, Murphy, BethAnn, Orth, Peter, Salowe, Scott, Shahripour, Aurash, Tracy, Rodger, Wang, Weixun, Wu, Chengwei, Xiong, Yusheng, Zokian, Hratch J, Wood, Harold B, Walji, Abbas

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Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor von Johns, Douglas G., Campeau, Louis-Charles, Banka, Puja, Bautmans, An, Bueters, Tjerk, Bianchi, Elisabetta, Branca, Danila, Bulger, Paul G., Crevecoeur, Inne, Ding, Fa-Xiang, Garbaccio, Robert M., Guetschow, Erik D., Guo, Yan, Ha, Sookhee N., Johnston, Jennifer M., Josien, Hubert, Kauh, Eunkyung A., Koeplinger, Kenneth A., Kuethe, Jeffrey T., Lai, Eseng, Lanning, Christine L., Lee, Anita Y.H., Li, Li, Nair, Anilkumar G., O’Neill, Edward A., Stoch, S. Aubrey, Thaisrivongs, David A., Tucker, Thomas J., Vachal, Petr, van Dyck, Kristien, Vanhoutte, Frederic P., Volckaert, Bram, Wolford, Dennis G., Xu, Andy, Zhao, Tian, Zhou, Dan, Zhou, Susan, Zhu, Xiaohong, Zokian, Hratch J., Walji, Abbas M., Wood, Harold B.

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Augmenting Hit Identification by Virtual Screening Techniques in Small Molecule Drug Discovery von Yan, Xin Cindy, Sanders, John M, Gao, Ying-Duo, Tudor, Matthew, Haidle, Andrew M, Klein, Daniel J, Converso, Antonella, Lesburg, Charles A, Zang, Yi, Wood, Harold B

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Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors von Keylor, Mitchell H, Gulati, Anmol, Kattar, Solomon D, Johnson, Rebecca E, Chau, Ryan W, Margrey, Kaila A, Ardolino, Michael J, Zarate, Cayetana, Poremba, Kelsey E, Simov, Vladimir, Morriello, Gregori J, Acton, John J, Pio, Barbara, Yan, Xin, Palte, Rachel L, McMinn, Spencer E, Nogle, Lisa, Lesburg, Charles A, Adpressa, Donovon, Lin, Shishi, Neelamkavil, Santhosh, Liu, Ping, Su, Jing, Hegde, Laxminarayan G, Woodhouse, Janice D, Faltus, Robert, Xiong, Tina, Ciaccio, Paul J, Piesvaux, Jennifer, Otte, Karin M, Wood, Harold B, Kennedy, Matthew E, Bennett, David Jonathan, DiMauro, Erin F, Fell, Matthew J, Fuller, Peter H

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Discovery and Optimization of N‑Heteroaryl Indazole LRRK2 Inhibitors von Logan, Kaitlyn M., Kaplan, Will, Simov, Vladimir, Zhou, Hua, Li, Derun, Torres, Luis, Morriello, Gregori J., Acton, John J., Pio, Barbara, Chen, Yi-Heng, Keylor, Mitchell H., Johnson, Rebecca, Kattar, Solomon D., Chau, Ryan, Yan, Xin, Ardolino, Michael, Zarate, Cayetana, Otte, Karin M., Palte, Rachel L., Xiong, Tina, McMinn, Spencer E., Lin, Shishi, Neelamkavil, Santhosh F., Liu, Ping, Su, Jing, Hegde, Laxminarayan G., Woodhouse, Janice D., Moy, Lily Y., Ciaccio, Paul J., Piesvaux, Jennifer, Zebisch, Matthias, Henry, Clare, Barker, John, Wood, Harold B., Kennedy, Matthew E., DiMauro, Erin F., Fell, Matthew J., Fuller, Peter H.

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Preclinical and translational evaluation of coagulation factor IXa as a novel therapeutic target von Ankrom, Wendy, Wood, Harold B., Xu, Jiayi, Geissler, Wayne, Bateman, Tom, Chatterjee, Manash S., Feng, Kung‐I, Metzger, Joseph M., Strapps, Walter R., Tadin‐Strapps, Marija, Seiffert, Dietmar, Andre, Patrick

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Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1‑Heteroaryl‑1H‑Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson’s Disease von Candito, David A., Simov, Vladimir, Gulati, Anmol, Kattar, Solomon, Chau, Ryan W., Lapointe, Blair T., Methot, Joey L., DeMong, Duane E., Graham, Thomas H., Kurukulasuriya, Ravi, Keylor, Mitchell H., Tong, Ling, Morriello, Gregori J., Acton, John J., Pio, Barbara, Liu, Weiguo, Scott, Jack D., Ardolino, Michael J., Martinot, Theodore A., Maddess, Matthew L., Yan, Xin, Gunaydin, Hakan, Palte, Rachel L., McMinn, Spencer E., Nogle, Lisa, Yu, Hongshi, Minnihan, Ellen C., Lesburg, Charles A., Liu, Ping, Su, Jing, Hegde, Laxminarayan G., Moy, Lily Y., Woodhouse, Janice D., Faltus, Robert, Xiong, Tina, Ciaccio, Paul, Piesvaux, Jennifer A., Otte, Karin M., Kennedy, Matthew E., Bennett, David Jonathan, DiMauro, Erin F., Fell, Matthew J., Neelamkavil, Santhosh, Wood, Harold B., Fuller, Peter H., Ellis, J. Michael

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Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants von Hussain, Zahid, Cooke, Andrew J., Neelamkavil, Santhosh, Brown, Lindsay, Carswell, Emma, Geissler, Wayne M., Guo, Zhuyan, Hawes, Brian, Kelly, Terri M., Kiyoi, Yasuko, Lai, KehDih, Lesburg, Charles, Pow, Eleanor, Zang, Yi, Wood, Harold B., Edmondson, Scott D., Liu, Weiguo

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Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1 H -Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease von Candito, David A, Simov, Vladimir, Gulati, Anmol, Kattar, Solomon, Chau, Ryan W, Lapointe, Blair T, Methot, Joey L, DeMong, Duane E, Graham, Thomas H, Kurukulasuriya, Ravi, Keylor, Mitchell H, Tong, Ling, Morriello, Gregori J, Acton, John J, Pio, Barbara, Liu, Weiguo, Scott, Jack D, Ardolino, Michael J, Martinot, Theodore A, Maddess, Matthew L, Yan, Xin, Gunaydin, Hakan, Palte, Rachel L, McMinn, Spencer E, Nogle, Lisa, Yu, Hongshi, Minnihan, Ellen C, Lesburg, Charles A, Liu, Ping, Su, Jing, Hegde, Laxminarayan G, Moy, Lily Y, Woodhouse, Janice D, Faltus, Robert, Xiong, Tina, Ciaccio, Paul, Piesvaux, Jennifer A, Otte, Karin M, Kennedy, Matthew E, Bennett, David Jonathan, DiMauro, Erin F, Fell, Matthew J, Neelamkavil, Santhosh, Wood, Harold B, Fuller, Peter H, Ellis, J Michael

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Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors von Sakurada, Isao, Endo, Toshiya, Hikita, Katsuyoshi, Hirabayashi, Tomokazu, Hosaka, Yoshitaka, Kato, Yutaka, Maeda, Yoshitaka, Matsumoto, Shigeki, Mizuno, Takashi, Nagasue, Hiroshi, Nishimura, Teruyuki, Shimada, Shunsuke, Shinozaki, Mikihiko, Taguchi, Keiko, Takeuchi, Katsutoshi, Yokoyama, Tooru, Hruza, Alan, Reichert, Paul, Zhang, Ting, Wood, Harold B., Nakao, Kazunari, Furusako, Shoji

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Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure–Activity Relationships and Guide D... von Zhang, Ting, Liu, Yong, Yang, Xianshu, Martin, Gary E, Yao, Huifang, Shang, Jackie, Bugianesi, Randal M, Ellsworth, Kenneth P, Sonatore, Lisa M, Nizner, Peter, Sherer, Edward C, Hill, Susan E, Knemeyer, Ian W, Geissler, Wayne M, Dandliker, Peter J, Helmy, Roy, Wood, Harold B

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Benzimidazolones: A New Class of Selective Peroxisome Proliferator-Activated Receptor γ (PPARγ) Modulators von Liu, Weiguo, Lau, Fiona, Liu, Kun, Wood, Harold B, Zhou, Gaochao, Chen, Yuli, Li, Ying, Akiyama, Taro E, Castriota, Gino, Einstein, Monica, Wang, Chualin, McCann, Margaret E, Doebber, Thomas W, Wu, Margaret, Chang, Ching H, McNamara, Lesley, McKeever, Brian, Mosley, Ralph T, Berger, Joel P, Meinke, Peter T

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Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors von Gulati, Anmol, Yeung, Charles S, Lapointe, Blair, Kattar, Solomon D, Gunaydin, Hakan, Scott, Jack D, Childers, Kaleen K, Methot, Joey L, Simov, Vladimir, Kurukulasuriya, Ravi, Pio, Barbara, Morriello, Greg J, Liu, Ping, Tang, Haiqun, Neelamkavil, Santhosh, Wood, Harold B, Rada, Vanessa L, Ardolino, Michael J, Yan, Xin Cindy, Palte, Rachel, Otte, Karin, Faltus, Robert, Woodhouse, Janice, Hegde, Laxminarayan G, Ciaccio, Paul, Minnihan, Ellen C, DiMauro, Erin F, Fell, Matthew J, Fuller, Peter H, Ellis, J. Michael

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Merck’s Reaction Review Policy: An Exercise in Process Safety von Bassan, Ephraim, Ruck, Rebecca T, Dienemann, Erik, Emerson, Khateeta M, Humphrey, Guy R, Raheem, Izzat T, Tschaen, David M, Vickery, Thomas P, Wood, Harold B, Yasuda, Nobuyoshi

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Discovery of phenyl acetamides as potent and selective GPR119 agonists von Zhu, Cheng, Wang, Liping, Zhu, Yuping, Guo, Zack Zhiqiang, Liu, Ping, Hu, Zhiyong, Szewczyk, Jason W., Kang, Ling, Chicchi, Gary, Ehrhardt, Anka, Woods, Andrea, Seo, Toru, Woods, Morgan, van Heek, Margaret, Dingley, Karen H., Pang, Jianmei, Salituro, Gino M., Powell, Joyce, Terebetski, Jenna L., Hornak, Viktor, Campeau, Louis-Charles, Orr, Robert K., Ujjainwalla, Feroze, Miller, Michael, Stamford, Andrew, Wood, Harold B., Kowalski, Timothy, Nargund, Ravi P., Edmondson, Scott D.

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Rapid development of two factor IXa inhibitors from hit to lead von Parker, Dann L., Walsh, Shawn, Li, Bing, Kim, Esther, Sharipour, Aurash, Smith, Cameron, Chen, Yi-Heng, Berger, Richard, Harper, Bart, Zhang, Ting, Park, Min, Shu, Min, Wu, Jane, Xu, Jiayi, Dewnani, Sunita, Sherer, Edward C., Hruza, Alan, Reichert, Paul, Geissler, Wayne, Sonatore, Lisa, Ellsworth, Kenneth, Balkovec, James, Greenlee, William, Wood, Harold B.

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Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5‑Selective Antagonists von Liu, Weiguo, Hussain, Zahid, Zang, Yi, Sweis, Ramzi F, Romero, F. Anthony, Finke, Paul E, Moningka, Remond, Bao, Jianming, Plotkin, Michael A, Shang, Jin, Dingley, Karen H, Salituro, Gino, Murphy, Beth Ann, Howard, Andrew D, Ujjainwalla, Feroze, Wood, Harold B, Duffy, Joseph L

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Development of a novel class of potent and selective FIXa inhibitors von Zhang, Ting, Andre, Patrick, Bateman, Thomas J., Chen, Yi-Heng, Desai, Kunal, Ellsworth, Kenneth, Geissler, Wayne M., Guo, Liangqin, Hruza, Alan, Jian, Tianying, Meng, Dongfang, Parker, Dann L., Qian, Xiaoxia, Reichert, Paul, Sherer, Edward C., Shu, Min, Smith, Cameron J., Sonatore, Lisa M., Tschirret-Guth, Richard, Nolting, Andrew F., Orr, Robert, Campeau, Louis-Charles, Araki, Kazuto, Nishimura, Teruyuki, Sakurada, Isao, Wood, Harold B.

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