Discovery of 7‑Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro‑1H‑indol-5-yl)‑7H‑pyrrolo[2,3‑d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inh... von Axten, Jeffrey M, Medina, Jesús R, Feng, Yanhong, Shu, Arthur, Romeril, Stuart P, Grant, Seth W, Li, William Hoi Hong, Heerding, Dirk A, Minthorn, Elisabeth, Mencken, Thomas, Atkins, Charity, Liu, Qi, Rabindran, Sridhar, Kumar, Rakesh, Hong, Xuan, Goetz, Aaron, Stanley, Thomas, Taylor, J. David, Sigethy, Scott D, Tomberlin, Ginger H, Hassell, Annie M, Kahler, Kirsten M, Shewchuk, Lisa M, Gampe, Robert T

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Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor von Dumble, Melissa, Crouthamel, Ming-Chih, Zhang, Shu-Yun, Schaber, Michael, Levy, Dana, Robell, Kimberly, Liu, Qi, Figueroa, David J, Minthorn, Elisabeth A, Seefeld, Mark A, Rouse, Meagan B, Rabindran, Sridhar K, Heerding, Dirk A, Kumar, Rakesh

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Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction von Gilmartin, Aidan G, Faitg, Thomas H, Richter, Mark, Groy, Arthur, Seefeld, Mark A, Darcy, Michael G, Peng, Xin, Federowicz, Kelly, Yang, Jingsong, Zhang, Shu-Yun, Minthorn, Elisabeth, Jaworski, Jon-Paul, Schaber, Michael, Martens, Stan, McNulty, Dean E, Sinnamon, Robert H, Zhang, Hong, Kirkpatrick, Robert B, Nevins, Neysa, Cui, Guanglei, Pietrak, Beth, Diaz, Elsie, Jones, Amber, Brandt, Martin, Schwartz, Benjamin, Heerding, Dirk A, Kumar, Rakesh

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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development von Axten, Jeffrey M, Romeril, Stuart P, Shu, Arthur, Ralph, Jeffrey, Medina, Jesús R, Feng, Yanhong, Li, William Hoi Hong, Grant, Seth W, Heerding, Dirk A, Minthorn, Elisabeth, Mencken, Thomas, Gaul, Nathan, Goetz, Aaron, Stanley, Thomas, Hassell, Annie M, Gampe, Robert T, Atkins, Charity, Kumar, Rakesh

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Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors von Horton, John R., Pathuri, Sarath, Wong, Kristen, Ren, Ren, Rueda, Lourdes, Fosbenner, David T., Heerding, Dirk A., McCabe, Michael T., Pappalardi, Melissa B., Zhang, Xing, King, Bryan W., Cheng, Xiaodong

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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells von Medina, Jesús R, Tian, Xinrong, Li, William H, Suarez, Dominic, Mack, James F, LaFrance, Louis, Martyr, Cuthbert, Brackley, James, Di Marco, Christina, Rivero, Ralph, Heerding, Dirk A, McHugh, Charles, Minthorn, Elisabeth, Bhaskar, Aishwarya, Rubin, Jacob, Butticello, Michael, Carpenter, Christopher, Nartey, Eldridge N, Berrodin, Thomas J, Kallal, Lorena A, Mangatt, Biju

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Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity von Concha, Nestor O, Smallwood, Angela, Bonnette, William, Totoritis, Rachel, Zhang, Guofeng, Federowicz, Kelly, Yang, Jingsong, Qi, Hongwei, Chen, Stephanie, Campobasso, Nino, Choudhry, Anthony E, Shuster, Leanna E, Evans, Karen A, Ralph, Jeff, Sweitzer, Sharon, Heerding, Dirk A, Buser, Carolyn A, Su, Dai-Shi, DeYoung, M Phillip

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1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI) von Heerding, Dirk A, Chan, George, DeWolf, Walter E, Fosberry, Andrew P, Janson, Cheryl A, Jaworski, Deborah D, McManus, Edward, Miller, William H, Moore, Terrance D, Payne, David J, Qiu, Xiayang, Rittenhouse, Stephen F, Slater-Radosti, Courtney, Smith, Ward, Takata, Dennis T, Vaidya, Kalindi S, Yuan, Catherine C.K, Huffman, William F

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Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity von RHODES, Nelson, HEERDING, Dirk A, KAHANA, Jason A, GESKE, Robert S, KIEYMENOVA, Elena V, CHOUDHRY, Anthony E, ZHIHONG LAI, LEBER, Jack D, MINTHORN, Elisabeth A, STRUM, Susan L, WOOD, Edgar R, HUANG, Pearl S, DUCKETT, Derek R, COPELAND, Robert A, KUMAR, Rakesh, EBERWEIN, Derek J, KNICK, Victoria B, LANSING, Timothy J, MCCONNELL, Randy T, GILMER, Tona M, ZHANG, Shu-Yun, ROBELL, Kimberly

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Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors von Su, Dai-Shi, Qu, Junya, Schulz, Mark, Blackledge, Chuck W, Yu, Hongyi, Zeng, Jenny, Burgess, Joelle, Reif, Alexander, Stern, Melissa, Nagarajan, Raman, Pappalardi, Melissa Baker, Wong, Kristen, Graves, Alan P, Bonnette, William, Wang, Liping, Elkins, Patricia, Knapp-Reed, Beth, Carson, Jeffrey D, McHugh, Charles, Mohammad, Helai, Kruger, Ryan, Luengo, Juan, Heerding, Dirk A, Creasy, Caretha L

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Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor... von Heerding, Dirk A, Rhodes, Nelson, Leber, Jack D, Clark, Tammy J, Keenan, Richard M, Lafrance, Louis V, Li, Mei, Safonov, Igor G, Takata, Dennis T, Venslavsky, Joseph W, Yamashita, Dennis S, Choudhry, Anthony E, Copeland, Robert A, Lai, Zhihong, Schaber, Michael D, Tummino, Peter J, Strum, Susan L, Wood, Edgar R, Duckett, Derek R, Eberwein, Derek, Knick, Victoria B, Lansing, Timothy J, McConnell, Randy T, Zhang, ShuYun, Minthorn, Elisabeth A, Concha, Nestor O, Warren, Gregory L, Kumar, Rakesh

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Aminofurazans as potent inhibitors of AKT kinase von Rouse, Meagan B., Seefeld, Mark A., Leber, Jack D., McNulty, Kenneth C., Sun, Lihui, Miller, William H., Zhang, ShuYun, Minthorn, Elisabeth A., Concha, Nestor O., Choudhry, Anthony E., Schaber, Michael D., Heerding, Dirk A.

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Discovery of a Novel and Potent Class of FabI-Directed Antibacterial Agents von PAYNE, David J, MILLER, William H, HEERDING, Dirk A, JANSON, Cheryl A, JAWORSKI, Deborah D, KELLER, Paul M, MANLEY, Peter J, MOORE, Terrance D, NEWLANDER, Kenneth A, PEARSON, Stewart, POLIZZI, Brian J, XIAYANG QIU, BERRY, Valerie, RITTENHOUSE, Stephen F, SLATER-RADOSTI, Courtney, SALYERS, Kevin L, SEEFELD, Mark A, SMYTH, Martin G, TAKATA, Dennis T, UZINSKAS, Irene N, VAIDYA, Kalindi, WALLIS, Nicola G, WINRAM, Scott B, BROSKY, John, YUAN, Catherine C. K, HUFFMAN, William F, BURGESS, Walter J, CHEN, Emile, DEWOLF, Walter E, FOSBERRY, Andrew P, GREENWOOD, Rebecca, HEAD, Martha S

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Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery von Medina, Jesús R, Blackledge, Charles W, Heerding, Dirk A, Campobasso, Nino, Ward, Paris, Briand, Jacques, Wright, Lois, Axten, Jeffrey M

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Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors von Seefeld, Mark A., Rouse, Meagan B., McNulty, Kenneth C., Sun, Lihui, Wang, Jizhou, Yamashita, Dennis S., Luengo, Juan I., Zhang, ShuYun, Minthorn, Elisabeth A., Concha, Nestor O., Heerding, Dirk A.

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Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI) von Miller, William H, Seefeld, Mark A, Newlander, Kenneth A, Uzinskas, Irene N, Burgess, Walter J, Heerding, Dirk A, Yuan, Catherine C. K, Head, Martha S, Payne, David J, Rittenhouse, Stephen F, Moore, Terrance D, Pearson, Stewart C, Berry, Valerie, DeWolf, Walter E, Keller, Paul M, Polizzi, Brian J, Qiu, Xiayang, Janson, Cheryl A, Huffman, William F

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2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles von Lin, Hong, Yamashita, Dennis S., Zeng, Jin, Xie, Ren, Verma, Sharad, Luengo, Juan I., Rhodes, Nelson, Zhang, Shuyun, Robell, Kimberly A., Choudhry, Anthony E., Lai, Zhihong, Kumar, Rakesh, Minthorn, Elisabeth A., Brown, Kristin K., Heerding, Dirk A.

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New benzimidazoles as thrombopoietin receptor agonists von Safonov, Igor G., Heerding, Dirk A., Keenan, Richard M., Price, Alan T., Erickson-Miller, Connie L., Hopson, Christopher B., Levin, Jenna L., Lord, Kenneth A., Tapley, Peter M.

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2,3,5-Trisubstituted pyridines as selective AKT inhibitors—Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity von Lin, Hong, Yamashita, Dennis S., Zeng, Jin, Xie, Ren, Wang, Wenyong, Nidarmarthy, Sirishkumar, Luengo, Juan I., Rhodes, Nelson, Knick, Victoria B., Choudhry, Anthony E., Lai, Zhihong, Minthorn, Elisabeth A., Strum, Susan L., Wood, Edgar R., Elkins, Patricia A., Concha, Nestor O., Heerding, Dirk A.

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Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines von Lin, Hong, Yamashita, Dennis S., Xie, Ren, Zeng, Jin, Wang, Wenyong, Leber, Jack, Safonov, Igor G., Verma, Sharad, Li, Mei, LaFrance, Louis, Venslavsky, Joseph, Takata, Dennis, Luengo, Juan I., Kahana, Jason A., Zhang, Shuyun, Robell, Kimberly A., Levy, Dana, Kumar, Rakesh, Choudhry, Anthony E., Schaber, Michael, Lai, Zhihong, Brown, Barry S., Donovan, Brian T., Minthorn, Elisabeth A., Brown, Kristin K., Heerding, Dirk A.

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