Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK) von Ott, Gregory R, Cheng, Mangeng, Learn, Keith S, Wagner, Jason, Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew, Mesaros, Eugen F, Ghose, Arup K, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Dobrzanski, Pawel, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin, Huang, Zeqi, Aimone, Lisa D, Bruckheimer, Elizabeth, Anderson, Nathan, Friedman, Jay, Fernandez, Sandra V, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

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Combined inhibition of atypical PKC and histone deacetylase 1 is cooperative in basal cell carcinoma treatment von Mirza, Amar N, Fry, Micah A, Urman, Nicole M, Atwood, Scott X, Roffey, Jon, Ott, Gregory R, Chen, Bin, Lee, Alex, Brown, Alexander S, Aasi, Sumaira Z, Hollmig, Tyler, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce R, Zificsak, Craig A, Sirota, Marina, Tang, Jean Y, Butte, Atul, Epstein, Ervin, Sarin, Kavita Y, Oro, Anthony E

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Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase von Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew A, Cheng, Mangeng, Quail, Matthew, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Haltiwanger, R. Curtis, Wells-Knecht, Kevin, Ott, Gregory R, Ghose, Arup K, Ator, Mark A, Ruggeri, Bruce, Dorsey, Bruce D

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Discovery and Process Synthesis of Novel 2,7-Pyrrolo[2,1-f][1,2,4]triazines von Thieu, Tho, Sclafani, Joseph A, Levy, Daniel V, McLean, Andrew, Breslin, Henry J, Ott, Gregory R, Bakale, Roger P, Dorsey, Bruce D

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Pyrrolo[2,1-f][1,2,4]triazines: From C-nucleosides to kinases and back again, the remarkable journey of a versatile nitrogen heterocycle von Ott, Gregory R., Favor, David A.

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Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors von Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D

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Technically Extended MultiParameter Optimization (TEMPO): An Advanced Robust Scoring Scheme To Calculate Central Nervous System Druggability and Monitor Lead Optimization von Ghose, Arup K, Ott, Gregory R, Hudkins, Robert L

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Structure-Based Drug Discovery of N‑((R)‑3-(7-Methyl‑1H‑indazol-5-yl)-1-oxo-1-(((S)‑1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2′-oxo... von Bucknell, Sarah J, Ator, Mark A, Brown, Alastair J. H, Brown, Jason, Cansfield, Andrew D, Cansfield, Julie E, Christopher, John A, Congreve, Miles, Cseke, Gabriella, Deflorian, Francesca, Jones, Christopher R, Mason, Jonathan S, O’Brien, M. Alistair, Ott, Gregory R, Pickworth, Mark, Southall, Stacey M

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Total Syntheses of (−)-Macrolactin A, (+)-Macrolactin E, and (−)-Macrolactinic Acid:  An Exercise in Stille Cross-Coupling Chemistry von Smith, Amos B, Ott, Gregory R

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The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells von Salem, Israa, Alsalahi, Manal, Chervoneva, Inna, Aburto, Lucy D, Addya, Sankar, Ott, Gregory R, Ruggeri, Bruce A, Cristofanilli, Massimo, Fernandez, Sandra V

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CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers von Cheng, Mangeng, Quail, Matthew R, Gingrich, Diane E, Ott, Gregory R, Lu, Lihui, Wan, Weihua, Albom, Mark S, Angeles, Thelma S, Aimone, Lisa D, Cristofani, Flavio, Machiorlatti, Rodolfo, Abele, Cristina, Ator, Mark A, Dorsey, Bruce D, Inghirami, Giorgio, Ruggeri, Bruce A

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Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein–Ligand Complexes von Cansfield, Andrew D, Ator, Mark A, Banerjee, Joydeep, Bestwick, Michael, Bortolato, Andrea, Brown, Giles A, Brown, Jason, Butkovic, Kristina, Cansfield, Julie E, Christopher, John A, Congreve, Miles, Cseke, Gabriella, Deflorian, Francesca, Dugan, Benjamin, Hunjadi, Martina Petrovic, Hutinec, Antun, Inturi, Trinadh Kumar, Landek, Goran, Mason, Jonathan, O’Brien, Alistair, Ott, Gregory R, Rupcic, Renata, Saxty, Gordon, Southall, Stacey M, Zadravec, Rahela, Watson, Stephen P

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Design, Synthesis, and Anaplastic Lymphoma Kinase (ALK) Inhibitory Activity for a Novel Series of 2,4,8,22-Tetraazatetracyclo[14.3.1.13,7.19,13]docosa-1(20),3(22),4,6,9(21),10,12,1... von Breslin, Henry J, Lane, Brandon M, Ott, Gregory R, Ghose, Arup K, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Wan, Weihua, Haltiwanger, R. Curtis, Wells-Knecht, Kevin J, Dorsey, Bruce D

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2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitu... von Ott, Gregory R, Wells, Gregory J, Thieu, Tho V, Quail, Matthew R, Lisko, Joseph G, Mesaros, Eugen F, Gingrich, Diane E, Ghose, Arup K, Wan, Weihua, Lu, Lihui, Cheng, Mangeng, Albom, Mark S, Angeles, Thelma S, Huang, Zeqi, Aimone, Lisa D, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase von Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Cheng, Mangeng, Ruggeri, Bruce A., Ator, Mark A., Dorsey, Bruce D., Ott, Gregory R.

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Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: Control of selectivity by a benzyloxy group von Tripathy, Rabindranath, McHugh, Robert J., Ghose, Arup K., Ott, Gregory R., Angeles, Thelma S., Albom, Mark S., Huang, Zeck, Aimone, Lisa D., Cheng, Mangeng, Dorsey, Bruce D.

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Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE): Discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1′ sub... von Lu, Zhonghui, Ott, Gregory R., Anand, Rajan, Liu, Rui-Qin, Covington, Maryanne B., Vaddi, Krishna, Qian, Mingxin, Newton, Robert C., Christ, David D., Trzaskos, James, Duan, James J.-W.

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Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models von Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., Dorsey, Bruce D.

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2,7-Disubstituted-Pyrrolotriazine Kinase Inhibitors with an Unusually High Degree of Reactive Metabolite Formation von Wells-Knecht, Kevin J, Ott, Gregory R, Cheng, Mangeng, Wells, Gregory J, Breslin, Henry J, Gingrich, Diane E, Weinberg, Linda, Mesaros, Eugen F, Huang, Zeqi, Yazdanian, Mehran, Ator, Mark A, Aimone, Lisa D, Zeigler, Kelli, Dorsey, Bruce D

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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors von Zificsak, Craig A, Theroff, Jay P, Aimone, Lisa D, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Mesaros, Eugen F, Ott, Gregory R, Quail, Matthew R, Underiner, Ted L, Wan, Weihua, Dorsey, Bruce D

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