Enhancer Activation by Pharmacologic Displacement of LSD1 from GFI1 Induces Differentiation in Acute Myeloid Leukemia von Maiques-Diaz, Alba, Spencer, Gary J., Lynch, James T., Ciceri, Filippo, Williams, Emma L., Amaral, Fabio M.R., Wiseman, Daniel H., Harris, William J., Li, Yaoyong, Sahoo, Sudhakar, Hitchin, James R., Mould, Daniel P., Fairweather, Emma E., Waszkowycz, Bohdan, Jordan, Allan M., Smith, Duncan L., Somervaille, Tim C.P.

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Outstanding challenges in protein-ligand docking and structure-based virtual screening von Waszkowycz, Bohdan, Clark, David E., Gancia, Emanuela

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Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sul... von Waszkowycz, Bohdan, Smith, Kate M, McGonagle, Alison E, Jordan, Allan M, Acton, Ben, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, James, Dominic I, Jones, Clifford D, Jones, Stuart, Mould, Daniel P, Small, Helen F, Stowell, Alexandra I. J, Tucker, Julie A, Waddell, Ian D, Ogilvie, Donald J

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Targeted genetic dependency screen facilitates identification of actionable mutations in FGFR4, MAP3K9, and PAK5 in lung cancer von Fawdar, Shameem, Trotter, Eleanor W., Li, Yaoyong, Stephenson, Natalie L., Hanke, Franziska, Marusiak, Anna A., Edwards, Zoe C., Ientile, Sara, Waszkowycz, Bohdan, Miller, Crispin J., Brognard, John

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Toxoflavins and Deazaflavins as the First Reported Selective Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase II von Raoof, Ali, Depledge, Paul, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hopkins, Gemma V, Jordan, Allan M, Maguire, Laura A, McGonagle, Alison E, Mould, Daniel P, Rushbrooke, Mathew, Small, Helen F, Smith, Kate M, Thomson, Graeme J, Turlais, Fabrice, Waddell, Ian D, Waszkowycz, Bohdan, Watson, Amanda J, Ogilvie, Donald J

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Towards improving compound selection in structure-based virtual screening von Waszkowycz, Bohdan

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Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade [version 1; peer revi... von Watson, Amanda J, Hopkins, Gemma V, Hitchin, Samantha, Begum, Habiba, Jones, Stuart, Jordan, Allan, Holt, Sarah, March, H. Nikki, Newton, Rebecca, Small, Helen, Stowell, Alex, Waddell, Ian D, Waszkowycz, Bohdan, Ogilvie, Donald J

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Identification of selective inhibitors of RET and comparison with current clinical candidates through development and validation of a robust screening cascade von Watson, Amanda J., Hopkins, Gemma V., Hitchin, Samantha, Begum, Habiba, Jones, Stuart, Jordan, Allan, Holt, Sarah, March, H. Nikki, Newton, Rebecca, Small, Helen, Stowell, Alex, Waddell, Ian D., Waszkowycz, Bohdan, Ogilvie, Donald J.

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First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib von James, Dominic I, Smith, Kate M, Jordan, Allan M, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, Jones, Stuart, Kelly, Paul, McGonagle, Alison E, Small, Helen, Stowell, Alexandra I. J, Tucker, Julie, Waddell, Ian D, Waszkowycz, Bohdan, Ogilvie, Donald J

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Protein Kinase Cδ Deficiency Causes Mendelian Systemic Lupus Erythematosus With B Cell‐Defective Apoptosis and Hyperproliferation von Belot, Alexandre, Kasher, Paul R., Trotter, Eleanor W., Foray, Anne‐Perrine, Debaud, Anne‐Laure, Rice, Gillian I., Szynkiewicz, Marcin, Zabot, Marie‐Therese, Rouvet, Isabelle, Bhaskar, Sanjeev S., Daly, Sarah B., Dickerson, Jonathan E., Mayer, Josephine, O'Sullivan, James, Juillard, Laurent, Urquhart, Jill E., Fawdar, Shameem, Marusiak, Anna A., Stephenson, Natalie, Waszkowycz, Bohdan, Beresford, Michael W., Biesecker, Leslie G., Black, Graeme C. M., René, Céline, Eliaou, Jean‐François, Fabien, Nicole, Ranchin, Bruno, Cochat, Pierre, Gaffney, Patrick M., Rozenberg, Flore, Lebon, Pierre, Malcus, Christophe, Crow, Yanick J., Brognard, John, Bonnefoy, Nathalie

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A reversed sulfonamide series of selective RORc inverse agonists von van Niel, Monique B., Fauber, Benjamin P., Cartwright, Matthew, Gaines, Simon, Killen, Jonathan C., René, Olivier, Ward, Stuart I., de Leon Boenig, Gladys, Deng, Yuzhong, Eidenschenk, Céline, Everett, Christine, Gancia, Emanuela, Ganguli, Arunima, Gobbi, Alberto, Hawkins, Julie, Johnson, Adam R., Kiefer, James R., La, Hank, Lockey, Peter, Norman, Maxine, Ouyang, Wenjun, Qin, Ann, Wakes, Nicole, Waszkowycz, Bohdan, Wong, Harvey

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Protein Kinase C[delta] Deficiency Causes Mendelian Systemic Lupus Erythematosus With B Cell-Defective Apoptosis and Hyperproliferation von Belot, Alexandre, Kasher, Paul R, Trotter, Eleanor W, ay, Anne-Perrine, Debaud, Anne-Laure, Rice, Gillian I, Szynkiewicz, Marcin, Zabot, Marie-Therese, Rouvet, Isabelle, Bhaskar, Sanjeev S, Daly, Sarah B, Dickerson, Jonathan E, Mayer, Josephine, O'Sullivan, James, Juillard, Laurent, Urquhart, Jill E, Fawdar, Shameem, Marusiak, Anna A, Stephenson, Natalie, Waszkowycz, Bohdan, W. Beresford, Michael, Biesecker, Leslie G, C. M. Black, Graeme, René, Céline, Eliaou, Jean-François, Fabien, Nicole, Ranchin, Bruno, Cochat, Pierre, Gaffney, Patrick M, Rozenberg, Flore, Lebon, Pierre, Malcus, Christophe, Crow, Yanick J, Brognard, John, Bonnefoy, Nathalie

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Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells von Jones, Stuart, Ahmet, Jonathan, Ayton, Kelly, Ball, Matthew, Cockerill, Mark, Fairweather, Emma, Hamilton, Nicola, Harper, Paul, Hitchin, James, Jordan, Allan, Levy, Colin, Lopez, Ruth, McKenzie, Eddie, Packer, Martin, Plant, Darren, Simpson, Iain, Simpson, Peter, Sinclair, Ian, Somervaille, Tim C. P, Small, Helen, Spencer, Gary J, Thomson, Graeme, Tonge, Michael, Waddell, Ian, Walsh, Jarrod, Waszkowycz, Bohdan, Wigglesworth, Mark, Wiseman, Daniel H, Ogilvie, Donald

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Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase von Newton, Rebecca, Waszkowycz, Bohdan, Seewooruthun, Chitra, Burschowsky, Daniel, Richards, Mark, Hitchin, Samantha, Begum, Habiba, Watson, Amanda, French, Eleanor, Hamilton, Niall, Jones, Stuart, Lin, Li-Ying, Waddell, Ian, Echalier, Aude, Bayliss, Richard, Jordan, Allan M, Ogilvie, Donald

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Identification of Imidazo-Pyrrolopyridines as Novel and Potent JAK1 Inhibitors von Kulagowski, Janusz J, Blair, Wade, Bull, Richard J, Chang, Christine, Deshmukh, Gauri, Dyke, Hazel J, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Harrison, Trevor K, Hewitt, Peter R, Liimatta, Marya, Hurley, Christopher A, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Bir Kohli, Pawan, Maxey, Robert J, Mendonca, Rohan, Mortara, Kyle, Murray, Jeremy, Narukulla, Raman, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, Ultsch, Mark, van Abbema, Anne, Ward, Stuart I, Waszkowycz, Bohdan, Zak, Mark

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Inhibiting NF-κB-inducing kinase (NIK): Discovery, structure-based design, synthesis, structure–activity relationship, and co-crystal structures von Li, Kexue, McGee, Lawrence R., Fisher, Ben, Sudom, Athena, Liu, Jinsong, Rubenstein, Steven M., Anwer, Mohmed K., Cushing, Timothy D., Shin, Youngsook, Ayres, Merrill, Lee, Fei, Eksterowicz, John, Faulder, Paul, Waszkowycz, Bohdan, Plotnikova, Olga, Farrelly, Ellyn, Xiao, Shou-Hua, Chen, Guoqing, Wang, Zhulun

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Application of virtual screening to the discovery of novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with potential for the treatment of cancer and axonopathies von Clark, David E., Waszkowycz, Bohdan, Wong, Melanie, Lockey, Peter M., Adalbert, Robert, Gilley, Jonathan, Clark, Jonathan, Coleman, Michael P.

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Abstract 3236: Delivering selective and cell-active inhibitors of V804M mutant RET kinase through structure-guided drug discovery von Jordan, Allan M., Newton, Rebecca, Waszkowycz, Bohdan, Bayliss, Richard, Begum, Habiba, Burschowsky, Daniel, Echalier, Aude, Hitchin, Samantha, Hutton, Colin, Johns, Shaun, Jones, Stuart, Lin, Li-Ying, Richards, Mark, Seewooruthun, Chitra, Stowell, Alex, Waddell, Ian, Watson, Mandy, Ogilvie, Donald

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The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity von Newton, Rebecca, Bowler, Katherine A., Burns, Emily M., Chapman, Philip J., Fairweather, Emma E., Fritzl, Samantha J.R., Goldberg, Kristin M., Hamilton, Niall M., Holt, Sarah V., Hopkins, Gemma V., Jones, Stuart D., Jordan, Allan M., Lyons, Amanda J., Nikki March, H., McDonald, Neil Q., Maguire, Laura A., Mould, Daniel P., Purkiss, Andrew G., Small, Helen F., Stowell, Alexandra I.J., Thomson, Graeme J., Waddell, Ian D., Waszkowycz, Bohdan, Watson, Amanda J., Ogilvie, Donald J.

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Abstract 2745: Pharmacological characterisation of cell active inhibitors of Poly(ADP-ribose) glycohydrolase (PARG) von James, Dominic, Jordan, Allan, Hamilton, Nicola, McGonagle, Alison, Smith, Kate, Stowell, Alexandra, Waddell, Ian, Waszkowycz, Bohdan, Ogilvie, Donald

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