Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies
Barlaam, Bernard, Casella, Robert, Cidado, Justin, Cook, Calum, De Savi, Chris, Dishington, Allan, Donald, Craig S, Drew, Lisa, Ferguson, Andrew D, Ferguson, Douglas, Glossop, Steve, Grebe, Tyler, Gu, Chungang, Hande, Sudhir, Hawkins, Janet, Hird, Alexander W, Holmes, Jane, Horstick, James, Jiang, Yun, Lamb, Michelle L, McGuire, Thomas M, Moore, Jane E, O’Connell, Nichole, Pike, Andy, Pike, Kurt G, Proia, Theresa, Roberts, Bryan, San Martin, Maryann, Sarkar, Ujjal, Shao, Wenlin, Stead, Darren, Sumner, Neil, Thakur, Kumar, Vasbinder, Melissa M, Varnes, Jeffrey G, Wang, Jianyan, Wang, Lei, Wu, Dedong, Wu, Liangwei, Yang, Bin, Yao, Tieguang
Published in Journal of medicinal chemistry (24.12.2020)
Published in Journal of medicinal chemistry (24.12.2020)
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Journal Article
A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants
Schenkel, Laurie B., Molina, Jennifer R., Swinger, Kerren K., Abo, Ryan, Blackwell, Danielle J., Lu, Alvin Z., Cheung, Anne E., Church, W. David, Kunii, Kaiko, Kuplast-Barr, Kristy G., Majer, Christina R., Minissale, Elena, Mo, Jan-Rung, Niepel, Mario, Reik, Christopher, Ren, Yue, Vasbinder, Melissa M., Wigle, Tim J., Richon, Victoria M., Keilhack, Heike, Kuntz, Kevin W.
Published in Cell chemical biology (19.08.2021)
Published in Cell chemical biology (19.08.2021)
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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 Kinase 1 Inhibitor
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
Published in Journal of medicinal chemistry (14.05.2020)
Published in Journal of medicinal chemistry (14.05.2020)
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Journal Article
Discovery of a Novel Class of Dimeric Smac Mimetics as Potent IAP Antagonists Resulting in a Clinical Candidate for the Treatment of Cancer (AZD5582)
Hennessy, Edward J, Adam, Ammar, Aquila, Brian M, Castriotta, Lillian M, Cook, Donald, Hattersley, Maureen, Hird, Alexander W, Huntington, Christopher, Kamhi, Victor M, Laing, Naomi M, Li, Danyang, MacIntyre, Terry, Omer, Charles A, Oza, Vibha, Patterson, Troy, Repik, Galina, Rooney, Michael T, Saeh, Jamal C, Sha, Li, Vasbinder, Melissa M, Wang, Haiyun, Whitston, David
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Journal Article
Discovery of a Series of 7‑Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement
Barlaam, Bernard, De Savi, Chris, Dishington, Allan, Drew, Lisa, Ferguson, Andrew D, Ferguson, Douglas, Gu, Chungang, Hande, Sudhir, Hassall, Lorraine, Hawkins, Janet, Hird, Alexander W, Holmes, Jane, Lamb, Michelle L, Lister, Andrew S, McGuire, Thomas M, Moore, Jane E, O’Connell, Nichole, Patel, Anil, Pike, Kurt G, Sarkar, Ujjal, Shao, Wenlin, Stead, Darren, Varnes, Jeffrey G, Vasbinder, Melissa M, Wang, Lei, Wu, Liangwei, Xue, Lin, Yang, Bin, Yao, Tieguang
Published in Journal of medicinal chemistry (28.10.2021)
Published in Journal of medicinal chemistry (28.10.2021)
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Journal Article
In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement
Wigle, Tim J, Blackwell, Danielle J, Schenkel, Laurie B, Ren, Yue, Church, W David, Desai, Hetvi J, Swinger, Kerren K, Santospago, Andrew G, Majer, Christina R, Lu, Alvin Z, Niepel, Mario, Perl, Nicholas R, Vasbinder, Melissa M, Keilhack, Heike, Kuntz, Kevin W
Published in Cell chemical biology (16.07.2020)
Published in Cell chemical biology (16.07.2020)
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Journal Article
Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule
Wigle, Tim J., Ren, Yue, Molina, Jennifer R., Blackwell, Danielle J., Schenkel, Laurie B., Swinger, Kerren K., Kuplast‐Barr, Kristy, Majer, Christina R., Church, W. David, Lu, Alvin Z., Mo, Jason, Abo, Ryan, Cheung, Anne, Dorsey, Bryan W., Niepel, Mario, Perl, Nicholas R., Vasbinder, Melissa M., Keilhack, Heike, Kuntz, Kevin W.
Published in Chembiochem : a European journal of chemical biology (15.06.2021)
Published in Chembiochem : a European journal of chemical biology (15.06.2021)
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Journal Article
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors
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
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Journal Article
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 Janus Kinase 1 Inhibitor
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
Published in Journal of medicinal chemistry (14.05.2020)
Published in Journal of medicinal chemistry (14.05.2020)
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Journal Article
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 Thiophenecarboxamide Ureas
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
Published in Journal of medicinal chemistry (14.06.2012)
Published in Journal of medicinal chemistry (14.06.2012)
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Journal Article
PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity
Gozgit, Joseph M., Vasbinder, Melissa M., Abo, Ryan P., Kunii, Kaiko, Kuplast-Barr, Kristy G., Gui, Bin, Lu, Alvin Z., Molina, Jennifer R., Minissale, Elena, Swinger, Kerren K., Wigle, Tim J., Blackwell, Danielle J., Majer, Christina R., Ren, Yue, Niepel, Mario, Varsamis, Zacharenia A., Nayak, Sunaina P., Bamberg, Ellen, Mo, Jan-Rung, Church, W. David, Mady, Ahmed S.A., Song, Jeff, Utley, Luke, Rao, Patricia E., Mitchison, Timothy J., Kuntz, Kevin W., Richon, Victoria M., Keilhack, Heike
Published in Cancer cell (13.09.2021)
Published in Cancer cell (13.09.2021)
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Journal Article
Identification of azabenzimidazoles as potent JAK1 selective inhibitors
Vasbinder, Melissa M., Alimzhanov, Marat, Augustin, Martin, Bebernitz, Geraldine, Bell, Kirsten, Chuaqui, Claudio, Deegan, Tracy, Ferguson, Andrew D., Goodwin, Kelly, Huszar, Dennis, Kawatkar, Aarti, Kawatkar, Sameer, Read, Jon, Shi, Jie, Steinbacher, Stefan, Steuber, Holger, Su, Qibin, Toader, Dorin, Wang, Haixia, Woessner, Richard, Wu, Allan, Ye, Minwei, Zinda, Michael
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
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Journal Article
Discovery and Optimization of a Novel Series of Potent Mutant B-Raf(V600E) Selective Kinase Inhibitors
Vasbinder, Melissa M., Aquila, Brian, Augustin, Martin, Chen, Huawei, Cheung, Tony, Cook, Donald, Drew, Lisa, Fauber, Benjamin P., Glossop, Steve, Grondine, Michael, Hennessy, Edward, Johannes, Jeffrey, Lee, Stephen, Lyne, Paul, Moertl, Mario, Omer, Charles, Palakurthi, Sangeetha, Pontz, Timothy, Read, Jon, Sha, Li, Shen, Minhui, Steinbacher, Stefan, Wang, Haixia, Wu, Allan, Ye, Minwei
Published in Journal of medicinal chemistry (14.03.2013)
Published in Journal of medicinal chemistry (14.03.2013)
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Journal Article
Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205
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
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes
Wigle, Tim J., Church, W. David, Majer, Christina R., Swinger, Kerren K., Aybar, Demet, Schenkel, Laurie B., Vasbinder, Melissa M., Brendes, Arne, Beck, Claudia, Prahm, Martin, Wegener, Dennis, Chang, Paul, Kuntz, Kevin W.
Published in SLAS discovery (01.03.2020)
Published in SLAS discovery (01.03.2020)
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Journal Article
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors
Janetka, James W., Almeida, Lynsie, Ashwell, Susan, Brassil, Patrick J., Daly, Kevin, Deng, Chun, Gero, Thomas, Glynn, Roberta E., Horn, Candice L., Ioannidis, Stephanos, Lyne, Paul, Newcombe, Nicholas J., Oza, Vibha B., Pass, Martin, Springer, Stephanie K., Su, Mei, Toader, Dorin, Vasbinder, Melissa M., Yu, Dingwei, Yu, Yan, Zabludoff, Sonya D.
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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