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 Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)
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
Published in Journal of medicinal chemistry (23.08.2012)
Published in Journal of medicinal chemistry (23.08.2012)
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Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
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
Published in Nature chemical biology (01.03.2014)
Published in Nature chemical biology (01.03.2014)
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Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor
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
Published in PloS one (30.06.2014)
Published in PloS one (30.06.2014)
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Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development
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
Published in ACS medicinal chemistry letters (10.10.2013)
Published in ACS medicinal chemistry letters (10.10.2013)
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Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors
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
Published in Structure (London) (02.06.2022)
Published in Structure (London) (02.06.2022)
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1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI)
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
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells
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
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity
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
Published in Molecular pharmacology (01.12.2015)
Published in Molecular pharmacology (01.12.2015)
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Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity
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
Published in Cancer research (Chicago, Ill.) (01.04.2008)
Published in Cancer research (Chicago, Ill.) (01.04.2008)
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Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors
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
Published in ACS medicinal chemistry letters (13.02.2020)
Published in ACS medicinal chemistry letters (13.02.2020)
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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 of AKT Kinase
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
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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Aminofurazans as potent inhibitors of AKT kinase
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.
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
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Discovery of a Novel and Potent Class of FabI-Directed Antibacterial Agents
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
Published in Antimicrobial Agents and Chemotherapy (01.10.2002)
Published in Antimicrobial Agents and Chemotherapy (01.10.2002)
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Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery
Medina, Jesús R, Blackledge, Charles W, Heerding, Dirk A, Campobasso, Nino, Ward, Paris, Briand, Jacques, Wright, Lois, Axten, Jeffrey M
Published in ACS medicinal chemistry letters (11.11.2010)
Published in ACS medicinal chemistry letters (11.11.2010)
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Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
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Discovery of Aminopyridine-Based Inhibitors of Bacterial Enoyl-ACP Reductase (FabI)
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
Published in Journal of medicinal chemistry (18.07.2002)
Published in Journal of medicinal chemistry (18.07.2002)
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2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles
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.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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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
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.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines
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.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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New benzimidazoles as thrombopoietin receptor agonists
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.
Published in Bioorganic & medicinal chemistry letters (01.03.2006)
Published in Bioorganic & medicinal chemistry letters (01.03.2006)
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