BRD4 amplification facilitates an oncogenic gene expression program in high-grade serous ovarian cancer and confers sensitivity to BET inhibitors von Rhyasen, Garrett W, Yao, Yi, Zhang, Jingwen, Dulak, Austin, Castriotta, Lillian, Jacques, Kelly, Zhao, Wei, Gharahdaghi, Farzin, Hattersley, Maureen M, Lyne, Paul D, Clark, Edwin, Zinda, Michael, Fawell, Stephen E, Mills, Gordon B, Chen, Huawei

Volltext

Accurate Prediction of the Relative Potencies of Members of a Series of Kinase Inhibitors Using Molecular Docking and MM-GBSA Scoring von Lyne, Paul D, Lamb, Michelle L, Saeh, Jamal C

Volltext

Structure-based virtual screening: an overview von Lyne, Paul D

Volltext

AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia von Keeton, Erika K., McEachern, Kristen, Dillman, Keith S., Palakurthi, Sangeetha, Cao, Yichen, Grondine, Michael R., Kaur, Surinder, Wang, Suping, Chen, Yuching, Wu, Allan, Shen, Minhui, Gibbons, Francis D., Lamb, Michelle L., Zheng, Xiaolan, Stone, Richard M., DeAngelo, Daniel J., Platanias, Leonidas C., Dakin, Les A., Chen, Huawei, Lyne, Paul D., Huszar, Dennis

Volltext

On Evaluating Molecular-Docking Methods for Pose Prediction and Enrichment Factors von Chen, Hongming, Lyne, Paul D, Giordanetto, Fabrizio, Lovell, Timothy, Li, Jin

Volltext

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies von Rhyasen, Garrett W, Hattersley, Maureen M, Yao, Yi, Dulak, Austin, Wang, Wenxian, Petteruti, Philip, Dale, Ian L, Boiko, Scott, Cheung, Tony, Zhang, Jingwen, Wen, Shenghua, Castriotta, Lillian, Lawson, Deborah, Collins, Michael, Bao, Larry, Ahdesmaki, Miika J, Walker, Graeme, O'Connor, Greg, Yeh, Tammie C, Rabow, Alfred A, Dry, Jonathan R, Reimer, Corinne, Lyne, Paul, Mills, Gordon B, Fawell, Stephen E, Waring, Michael J, Zinda, Michael, Clark, Edwin, Chen, Huawei

Volltext

STAT3 antisense oligonucleotide AZD9150 in a subset of patients with heavily pretreated lymphoma: results of a phase 1b trial von Reilley, Matthew J, McCoon, Patricia, Cook, Carl, Lyne, Paul, Kurzrock, Razelle, Kim, Youngsoo, Woessner, Richard, Younes, Anas, Nemunaitis, John, Fowler, Nathan, Curran, Michael, Liu, Qinying, Zhou, Tianyuan, Schmidt, Joanna, Jo, Minji, Lee, Samantha J, Yamashita, Mason, Hughes, Steven G, Fayad, Luis, Piha-Paul, Sarina, Nadella, Murali V P, Xiao, Xiaokun, Hsu, Jeff, Revenko, Alexey, Monia, Brett P, MacLeod, A Robert, Hong, David S

Volltext

Discovery of (2R)‑N‑[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]‑1H‑indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kin... von Su, Qibin, Banks, Erica, Bebernitz, Geraldine, Bell, Kirsten, Borenstein, Cassandra F, Chen, Huawei, Chuaqui, Claudio E, Deng, Nanhua, Ferguson, Andrew D, Kawatkar, Sameer, Grimster, Neil P, Ruston, Linette, Lyne, Paul D, Read, Jon A, Peng, Xianyou, Pei, Xiaohui, Fawell, Stephen, Tang, Zhanlei, Throner, Scott, Vasbinder, Melissa M, Wang, Haoyu, Winter-Holt, Jon, Woessner, Richard, Wu, Allan, Yang, Wenzhan, Zinda, Michael, Kettle, Jason G

Volltext

Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases von Dakin, Les A., Block, Michael H., Chen, Huawei, Code, Erin, Dowling, James E., Feng, Xiaomei, Ferguson, Andrew D., Green, Isabelle, Hird, Alexander W., Howard, Tina, Keeton, Erika K., Lamb, Michelle L., Lyne, Paul D., Pollard, Hannah, Read, Jon, Wu, Allan J., Zhang, Tao, Zheng, Xiaolan

Volltext

Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer von Wang, Zebin, Grosskurth, Shaun E, Cheung, Tony, Petteruti, Philip, Zhang, Jingwen, Wang, Xin, Wang, Wenxian, Gharahdaghi, Farzin, Wu, Jiaquan, Su, Nancy, Howard, Ryan T, Mayo, Michele, Widzowski, Dan, Scott, David A, Johannes, Jeffrey W, Lamb, Michelle L, Lawson, Deborah, Dry, Jonathan R, Lyne, Paul D, Tate, Edward W, Zinda, Michael, Mikule, Keith, Fawell, Stephen E, Reimer, Corinne, Chen, Huawei

Volltext

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors von Yang, Bin, Vasbinder, Melissa M, Hird, Alexander W, Su, Qibin, Wang, Haixia, Yu, Yan, Toader, Dorin, Lyne, Paul D, Read, Jon A, Breed, Jason, Ioannidis, Stephanos, Deng, Chun, Grondine, Michael, DeGrace, Nancy, Whitston, David, Brassil, Patrick, Janetka, James W

Volltext

Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering von Johannes, Jeffrey W., Almeida, Lynsie, Daly, Kevin, Ferguson, Andrew D., Grosskurth, Shaun E., Guan, Huiping, Howard, Tina, Ioannidis, Stephanos, Kazmirski, Steven, Lamb, Michelle L., Larsen, Nicholas A., Lyne, Paul D., Mikule, Keith, Ogoe, Claude, Peng, Bo, Petteruti, Philip, Read, Jon A., Su, Nancy, Sylvester, Mark, Throner, Scott, Wang, Wenxian, Wang, Xin, Wu, Jiaquan, Ye, Qing, Yu, Yan, Zheng, Xiaolan, Scott, David A.

Volltext

Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer von Revenko, Alexey, Carnevalli, Larissa S, Sinclair, Charles, Johnson, Ben, Peter, Alison, Taylor, Molly, Hettrick, Lisa, Chapman, Melissa, Klein, Stephanie, Solanki, Anisha, Gattis, Danielle, Watt, Andrew, Hughes, Adina M, Magiera, Lukasz, Kar, Gozde, Ireland, Lucy, Mele, Deanna A, Sah, Vasu, Singh, Maneesh, Walton, Josephine, Mairesse, Maelle, King, Matthew, Edbrooke, Mark, Lyne, Paul, Barry, Simon T, Fawell, Stephen, Goldberg, Frederick W, MacLeod, A Robert

Volltext

Discovery of (2 R )- N -[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H -indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Jan... von Su, Qibin, Banks, Erica, Bebernitz, Geraldine, Bell, Kirsten, Borenstein, Cassandra F, Chen, Huawei, Chuaqui, Claudio E, Deng, Nanhua, Ferguson, Andrew D, Kawatkar, Sameer, Grimster, Neil P, Ruston, Linette, Lyne, Paul D, Read, Jon A, Peng, Xianyou, Pei, Xiaohui, Fawell, Stephen, Tang, Zhanlei, Throner, Scott, Vasbinder, Melissa M, Wang, Haoyu, Winter-Holt, Jon, Woessner, Richard, Wu, Allan, Yang, Wenzhan, Zinda, Michael, Kettle, Jason G

Volltext

Discovery of Checkpoint Kinase Inhibitor (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by Structure-Based Design and Optimization of Thiophene... von Oza, Vibha, Ashwell, Susan, Almeida, Lynsie, Brassil, Patrick, Breed, Jason, Deng, Chun, Gero, Thomas, Grondine, Michael, Horn, Candice, Ioannidis, Stephanos, Liu, Dongfang, Lyne, Paul, Newcombe, Nicholas, Pass, Martin, Read, Jon, Ready, Shannon, Rowsell, Siân, Su, Mei, Toader, Dorin, Vasbinder, Melissa, Yu, Dingwei, Yu, Yan, Xue, Yafeng, Zabludoff, Sonya, Janetka, James

Volltext

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases von Gingipalli, Lakshmaiah, Block, Michael H., Bao, Larry, Cooke, Emma, Dakin, Les A., Denz, Christopher R., Ferguson, Andrew D., Johannes, Jeffrey W., Larsen, Nicholas A., Lyne, Paul D., Pontz, Timothy W., Wang, Tao, Wu, Xiaoyun, Wu, Allan, Zhang, Hai-Jun, Zheng, Xiaolan, Dowling, James E., Lamb, Michelle L.

Volltext

Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering von Gu, Chungang, Lamb, Michelle L., Johannes, Jeffrey W., Sylvester, Mark A., Eisman, Mark S., Harrison, Rane A., Hu, Haiqing, Kazmirski, Steven, Mikule, Keith, Peng, Bo, Su, Nancy, Wang, Wenxian, Ye, Qing, Zheng, Xiaolan, Lyne, Paul D., Scott, David A.

Volltext

Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo von Dowling, James E, Alimzhanov, Marat, Bao, Larry, Chuaqui, Claudio, Denz, Christopher R, Jenkins, Emma, Larsen, Nicholas A, Lyne, Paul D, Pontz, Timothy, Ye, Qing, Holdgate, Geoff A, Snow, Lindsay, O’Connell, Nichole, Ferguson, Andrew D

Volltext

Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205 von Kettle, Jason G., Su, Qibin, Grimster, Neil, Kawatkar, Sameer, Throner, Scott, Woessner, Richard, Chen, Huawei, Bebernitz, Geraldine, Bell, Kristen, Anderson, Erica, Ruston, Linette, Winter-Holt, Jon, Lyne, Paul, Vasbinder, Melissa, Chuaqui, Claudio

Volltext

Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases von Wang, Tao, Lamb, Michelle L, Scott, David A, Wang, Haixia, Block, Michael H, Lyne, Paul D, Lee, John W, Davies, Audrey M, Zhang, Hai-Jun, Zhu, Yanyi, Gu, Fei, Han, Yongxin, Wang, Bin, Mohr, Peter J, Kaus, Robert J, Josey, John A, Hoffmann, Ethan, Thress, Ken, MacIntyre, Terry, Wang, Haiyun, Omer, Charles A, Yu, Dingwei

Volltext