Identification of the Clinical Candidate PF-07284890 (ARRY-461), a Highly Potent and Brain Penetrant BRAF Inhibitor for the Treatment of Cancer von Ren, Li, Moreno, David, Baer, Brian R., Barbour, Patrick, Bettendorf, Tanna, Bouhana, Karyn, Brown, Karin, Brown, Suzy A., Fell, Jay B., Hartley, Dylan P., Hicken, Erik J., Laird, Ellen R., Lee, Patrice, McCown, Joseph, Otten, Jennifer N., Prigaro, Brett, Wallace, Ross, Kahn, Dean

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SHP2 Inhibition Sensitizes Diverse Oncogene-Addicted Solid Tumors to Re-treatment with Targeted Therapy von Drilon, Alexander, Sharma, Manish R, Johnson, Melissa L, Yap, Timothy A, Gadgeel, Shirish, Nepert, Dale, Feng, Gang, Reddy, Micaela B, Harney, Allison S, Elsayed, Mohamed, Cook, Adam W, Wong, Christina E, Hinklin, Ronald J, Jiang, Yutong, Brown, Eric N, Neitzel, Nickolas A, Laird, Ellen R, Wu, Wen-I, Singh, Anurag, Wei, Ping, Ching, Keith A, Gaudino, John J, Lee, Patrice A, Hartley, Dylan P, Rothenberg, S Michael

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Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA von Hicken, Erik J., Brown, Karin, Dwulet, Natalie C., Gaudino, John J., Hansen, Erik P., Hartley, Dylan P., Kowalski, John P., Laird, Ellen R., Lazzara, Nicholas C., Li, Bin, Mou, Tung-Chung, Mutryn, Marie F., Oko, Lauren, Pajk, Spencer, Pipal, Robert W., Rosen, Rachel Z., Shelp, Russell, Singh, Anurag, Wang, Jing, Wise, Courtney E., Wong, Christina, Wong, Jim Y.

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Discovery of Potent and Selective Covalent Inhibitors of HER2 WT and HER2 YVMA von Hicken, Erik J, Brown, Karin, Dwulet, Natalie C, Gaudino, John J, Hansen, Erik P, Hartley, Dylan P, Kowalski, John P, Laird, Ellen R, Lazzara, Nicholas C, Li, Bin, Mou, Tung-Chung, Mutryn, Marie F, Oko, Lauren, Pajk, Spencer, Pipal, Robert W, Rosen, Rachel Z, Shelp, Russell, Singh, Anurag, Wang, Jing, Wise, Courtney E, Wong, Christina, Wong, Jim Y

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Discovery of Pyrazolopyrazines as Selective, Potent, and Mutant-Active MET Inhibitors with Intracranial Efficacy von Bumpers, Quinn A., Pipal, Robert W., Benz-Weeden, Anna M., Brewster, James T., Cook, Adam, Crooks, Amy L., Cruz, Cole, Dwulet, Natalie C., Gaudino, John J., Golec, Daniel, Harrison, Jacqueline A., Hartley, Dylan P., Hassanien, Sherif H., Hicken, Erik J., Kahn, Dean, Laird, Ellen R., Lemieux, Christine, Lewandowski, Nicholas, McCown, Joseph, McDonald, Matthew G., McNulty, Oren, Mou, Tung-Chung, Nguyen, Phong, Oko, Lauren, Opie, Lisa Pieti, Otten, Jennifer, Peck, Spencer C., Polites, Viktor C., Randall, Samuel D., Rosen, Rachel Z., Savechenkov, Pavel, Simpson, Helen, Singh, Anurag, Sparks, Drew, Wickersham, Kyle, Wollenberg, Lance, Wong, Christina E., Wong, Jim, Wu, Wen-I, Elsayed, Mohamed S. A., Hinklin, Ronald J., Tang, Tony P.

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Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase von Newhouse, Bradley J., Wenglowsky, Steve, Grina, Jonas, Laird, Ellen R., Voegtli, Walter C., Ren, Li, Ahrendt, Kateri, Buckmelter, Alex, Gloor, Susan L., Klopfenstein, Nathalie, Rudolph, Joachim, Wen, Zhaoyang, Li, Xianfeng, Feng, Bainian

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Pyrazolopyridine inhibitors of B-RafV600E. Part 2: Structure–activity relationships von Wenglowsky, Steve, Ahrendt, Kateri A., Buckmelter, Alex J., Feng, Bainian, Gloor, Susan L., Gradl, Stefan, Grina, Jonas, Hansen, Joshua D., Laird, Ellen R., Lunghofer, Paul, Mathieu, Simon, Moreno, David, Newhouse, Brad, Ren, Li, Risom, Tyler, Rudolph, Joachim, Seo, Jeongbeob, Sturgis, Hillary L., Voegtli, Walter C., Wen, Zhaoyang

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Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors von Shiozaki, Makoto, Maeda, Katsuya, Miura, Tomoya, Kotoku, Masayuki, Yamasaki, Takayuki, Matsuda, Isamu, Aoki, Kenta, Yasue, Katsutaka, Imai, Hiroto, Ubukata, Minoru, Suma, Akira, Yokota, Masahiro, Hotta, Takahiro, Tanaka, Masahiro, Hase, Yasunori, Haas, Julia, Fryer, Andrew M, Laird, Ellen R, Littmann, Nicole M, Andrews, Steven W, Josey, John A, Mimura, Takayuki, Shinozaki, Yuichi, Yoshiuchi, Hiromi, Inaba, Takashi

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Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors von Wenglowsky, Steve, Moreno, David, Laird, Ellen R, Gloor, Susan L, Ren, Li, Risom, Tyler, Rudolph, Joachim, Sturgis, Hillary L, Voegtli, Walter C

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Potent and Selective Aminopyrimidine-Based B-Raf Inhibitors with Favorable Physicochemical and Pharmacokinetic Properties von Mathieu, Simon, Gradl, Stefan N, Ren, Li, Wen, Zhaoyang, Aliagas, Ignacio, Gunzner-Toste, Janet, Lee, Wendy, Pulk, Rebecca, Zhao, Guiling, Alicke, Bruno, Boggs, Jason W, Buckmelter, Alex J, Choo, Edna F, Dinkel, Victoria, Gloor, Susan L, Gould, Stephen E, Hansen, Joshua D, Hastings, Gregg, Hatzivassiliou, Georgia, Laird, Ellen R, Moreno, David, Ran, Yingqing, Voegtli, Walter C, Wenglowsky, Steve, Grina, Jonas, Rudolph, Joachim

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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase von Wenglowsky, Steve, Ren, Li, Grina, Jonas, Hansen, Joshua D, Laird, Ellen R, Moreno, David, Dinkel, Victoria, Gloor, Susan L, Hastings, Gregg, Rana, Sumeet, Rasor, Kevin, Sturgis, Hillary L, Voegtli, Walter C, Vigers, Guy, Willis, Brandon, Mathieu, Simon, Rudolph, Joachim

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Non-oxime pyrazole based inhibitors of B-Raf kinase von Newhouse, Bradley J., Hansen, Joshua D., Grina, Jonas, Welch, Mike, Topalov, George, Littman, Nicole, Callejo, Michele, Martinson, Matthew, Galbraith, Sarah, Laird, Ellen R., Brandhuber, Barbara J., Vigers, Guy, Morales, Tony, Woessner, Rich, Randolph, Nikole, Lyssikatos, Joseph, Olivero, Alan

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Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties von Ren, Li, Laird, Ellen R, Buckmelter, Alex J, Dinkel, Victoria, Gloor, Susan L, Grina, Jonas, Newhouse, Brad, Rasor, Kevin, Hastings, Gregg, Gradl, Stefan N, Rudolph, Joachim

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Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors von Eary, C. Todd, Jones, Zachary S., Groneberg, Robert D., Burgess, Laurence E., Mareska, David A., Drew, Mark D., Blake, James F., Laird, Ellen R., Balachari, Devan, O’Sullivan, Michael, Allen, Andrew, Marsh, Vivienne

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Non-oxime inhibitors of B-Raf(V600E) kinase von Ren, Li, Wenglowsky, Steve, Miknis, Greg, Rast, Bryson, Buckmelter, Alex J, Ely, Robert J, Schlachter, Stephen, Laird, Ellen R, Randolph, Nikole, Callejo, Michele, Martinson, Matthew, Galbraith, Sarah, Brandhuber, Barbara J, Vigers, Guy, Morales, Tony, Voegtli, Walter C, Lyssikatos, Joseph

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Theoretical and Experimental Design of Atypical Kinase Inhibitors:  Application to p38 MAP Kinase von McClure, Kim F, Abramov, Yuriy A, Laird, Ellen R, Barberia, John T, Cai, Weiling, Carty, Thomas J, Cortina, Santo R, Danley, Dennis E, Dipesa, Alan J, Donahue, Kathleen M, Dombroski, Mark A, Elliott, Nancy C, Gabel, Christopher A, Han, Seungil, Hynes, Thomas R, LeMotte, Peter K, Mansour, Mahmoud N, Marr, Eric S, Letavic, Michael A, Pandit, Jayvardhan, Ripin, David B, Sweeney, Francis J, Tan, Douglas, Tao, Yong

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The Discovery of furo[2,3- c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors von Buckmelter, Alex J., Ren, Li, Laird, Ellen R., Rast, Bryson, Miknis, Greg, Wenglowsky, Steve, Schlachter, Stephen, Welch, Mike, Tarlton, Eugene, Grina, Jonas, Lyssikatos, Joseph, Brandhuber, Barbara J., Morales, Tony, Randolph, Nikole, Vigers, Guy, Martinson, Matthew, Callejo, Michele

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Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors von Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A, Laird, Ellen R, Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J, Choo, Edna F, Dinkel, Victoria, Feng, Bainian, Gloor, Susan L, Gould, Stephen E, Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D, Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J, Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T, Shrag, Michael, Song, Kyung, Sturgis, Hillary L, Voegtli, Walter C, Wen, Zhaoyang, Willis, Brandon S, Woessner, Richard D, Wu, Wen-I, Young, Wendy B, Grina, Jonas

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Pyrazolopyridine inhibitors of B-RafV600E. Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors von Wenglowsky, Steve, Moreno, David, Laird, Ellen R., Gloor, Susan L., Ren, Li, Risom, Tyler, Rudolph, Joachim, Sturgis, Hillary L., Voegtli, Walter C.

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Octahydrophenanthrene-2,7-diol Analogues as Dissociated Glucocorticoid Receptor Agonists: Discovery and Lead Exploration von Robinson, Ralph P, Buckbinder, Leonard, Haugeto, Amber I, McNiff, Patricia A, Millham, Michele L, Reese, Matthew R, Schaefer, Jean F, Abramov, Yuriy A, Bordner, Jon, Chantigny, Yves A, Kleinman, Edward F, Laird, Ellen R, Morgan, Bradley P, Murray, John C, Salter, Eben D, Wessel, Matthew D, Yocum, Sue A

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