Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients
Yuda, Junichiro, Will, Christine, Phillips, Darren C., Abraham, Linu, Alvey, Cory, Avigdor, Abraham, Buck, Wayne, Besenhofer, Lauren, Boghaert, Erwin, Cheng, Dong, Cojocari, Dan, Doyle, Kelly, Hansen, T. Matthew, Huang, Kevin, Johnson, Eric F., Judd, Andrew S., Judge, Russell A., Kalvass, John C., Kunzer, Aaron, Lam, Lloyd T., Li, Rachel, Martin, Ruth L., Mastracchio, Anthony, Mitten, Mike, Petrich, Adam, Wang, Jin, Ward, James E., Zhang, Haichao, Wang, Xilu, Wolff, Johannes E., Bell-McGuinn, Katherine M., Souers, Andrew J.
Published in Communications medicine (25.10.2023)
Published in Communications medicine (25.10.2023)
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Journal Article
Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor
Zhao, Gang, Souers, Andrew J, Voorbach, Martin, Falls, H. Doug, Droz, Brian, Brodjian, Sevan, Lau, Yau Yi, Iyengar, Rajesh R, Gao, Ju, Judd, Andrew S, Wagaw, Seble H, Ravn, Matthew M, Engstrom, Kenneth M, Lynch, John K, Mulhern, Mathew M, Freeman, Jennifer, Dayton, Brian D, Wang, Xiaojun, Grihalde, Nelson, Fry, Dennis, Beno, David W. A, Marsh, Kennan C, Su, Zhi, Diaz, Gilbert J, Collins, Christine A, Sham, Hing, Reilly, Regina M, Brune, Michael E, Kym, Philip R
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
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Journal Article
Identification and Preliminary Characterization of a Potent, Safe, and Orally Efficacious Inhibitor of Acyl-CoA:Diacylglycerol Acyltransferase 1
Yeh, Vince S. C, Beno, David W. A, Brodjian, Sevan, Brune, Michael E, Cullen, Steven C, Dayton, Brian D, Dhaon, Madhup K, Falls, Hugh D, Gao, Ju, Grihalde, Nelson, Hajduk, Philip, Hansen, T. Matthew, Judd, Andrew S, King, Andrew J, Klix, Russel C, Larson, Kelly J, Lau, Yau Y, Marsh, Kennan C, Mittelstadt, Scott W, Plata, Dan, Rozema, Michael J, Segreti, Jason A, Stoner, Eric J, Voorbach, Martin J, Wang, Xiaojun, Xin, Xili, Zhao, Gang, Collins, Christine A, Cox, Bryan F, Reilly, Regina M, Kym, Philip R, Souers, Andrew J
Published in Journal of medicinal chemistry (23.02.2012)
Published in Journal of medicinal chemistry (23.02.2012)
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Discovery of ((4R,5S)-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a Highly Potent, Selective, Orally Efficacious, and Safe Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Pei, Zhonghua, Li, Xiaofeng, von Geldern, Thomas W, Madar, David J, Longenecker, Kenton, Yong, Hong, Lubben, Thomas H, Stewart, Kent D, Zinker, Bradley A, Backes, Bradley J, Judd, Andrew S, Mulhern, Mathew, Ballaron, Stephen J, Stashko, Michael A, Mika, Amanda K, Beno, David W. A, Reinhart, Glenn A, Fryer, Ryan M, Preusser, Lee C, Kempf-Grote, Anita J, Sham, Hing L, Trevillyan, James M
Published in Journal of medicinal chemistry (02.11.2006)
Published in Journal of medicinal chemistry (02.11.2006)
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Journal Article
Discovery and Characterization of Aminopiperidinecoumarin Melanin Concentrating Hormone Receptor 1 Antagonists
Kym, Philip R, Iyengar, Rajesh, Souers, Andrew J, Lynch, John K, Judd, Andrew S, Gao, Ju, Freeman, Jennifer, Mulhern, Mathew, Zhao, Gang, Vasudevan, Anil, Wodka, Dariusz, Blackburn, Christopher, Brown, Jim, Che, Jennifer Lee, Cullis, Courtney, Lai, Su Jen, LaMarche, Matthew J, Marsilje, Tom, Roses, Jon, Sells, Todd, Geddes, Brad, Govek, Elizabeth, Patane, Michael, Fry, Dennis, Dayton, Brian D, Brodjian, Sevan, Falls, Doug, Brune, Michael, Bush, Eugene, Shapiro, Robin, Knourek-Segel, Victoria, Fey, Thomas, McDowell, Cathleen, Reinhart, Glenn A, Preusser, Lee C, Marsh, Kennan, Hernandez, Lisa, Sham, Hing L, Collins, Christine A
Published in Journal of medicinal chemistry (22.09.2005)
Published in Journal of medicinal chemistry (22.09.2005)
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Enantioselective Bioreduction of Medicinally Relevant Nitrogen-Heteroaromatic Ketones
Bai, Wen-Ju, Estrada, Michelle A., Gartman, Jackson A., Judd, Andrew S.
Published in ACS medicinal chemistry letters (08.06.2023)
Published in ACS medicinal chemistry letters (08.06.2023)
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Journal Article
Enabling, Decagram-Scale Synthesis of Macrocyclic MCL‑1 Inhibitor ABBV-467
Brady, Patrick B., Sorensen, Bryan K., Risi, Roberto M., Curtin, Michael L., Mantei, Robert A., Florjancic, Alan S., Mastracchio, Anthony, Ji, Cheng, Kunzer, Aaron R., Lai, Chunqiu, Storer, Gregory E., Chan, Vincent S., Henry, Rodger F., Souers, Andrew J., Michaelides, Michael R., Judd, Andrew S., Hansen, T. Matthew
Published in Journal of organic chemistry (17.11.2023)
Published in Journal of organic chemistry (17.11.2023)
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Structure-Based Design of A-1293102, a Potent and Selective BCL-X-L Inhibitor
Tao, Zhi-Fu, Wang, Xilu, Chen, Jun, Ingram, Justin P., Jin, Sha, Judge, Russell A., Kovar, Peter J., Park, Chang, Sun, Chaohong, Wakefield, Brian D., Zhou, Li, Zhang, Haichao, Elmore, Steven W., Phillips, Darren C., Judd, Andrew S., Leverson, Joel D., Souers, Andrew J.
Published in ACS medicinal chemistry letters (10.06.2021)
Published in ACS medicinal chemistry letters (10.06.2021)
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Journal Article
Structure-Based Design of A‑1293102, a Potent and Selective BCL‑XL Inhibitor
Tao, Zhi-Fu, Wang, Xilu, Chen, Jun, Ingram, Justin P, Jin, Sha, Judge, Russell A, Kovar, Peter J, Park, Chang, Sun, Chaohong, Wakefield, Brian D, Zhou, Li, Zhang, Haichao, Elmore, Steven W, Phillips, Darren C, Judd, Andrew S, Leverson, Joel D, Souers, Andrew J
Published in ACS medicinal chemistry letters (10.06.2021)
Published in ACS medicinal chemistry letters (10.06.2021)
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Journal Article
BCL-XL-targeting antibody-drug conjugates are active in preclinical models and mitigate on-mechanism toxicity of small-molecule inhibitors
Judd, Andrew S, Bawa, Bhupinder, Buck, Wayne R, Tao, Zhi-Fu, Li, Yingchun, Mitten, Michael J, Bruncko, Milan, Catron, Nathaniel, Doherty, George, Durbin, Kenneth R, Enright, Brian, Frey, Robin, Haasch, Deanna, Haman, Sandra, Haight, Anthony R, Henriques, Tracy A, Holms, James, Izeradjene, Kamel, Judge, Russell A, Jenkins, Gary J, Kunzer, Aaron, Leverson, Joel D, Martin, Ruth L, Mitra, Diya, Mittelstadt, Scott, Nelson, Lorne, Nimmer, Paul, Palma, Joann, Peterson, Richard, Phillips, Darren C, Ralston, Sherry L, Rosenberg, Saul H, Shen, Xiaoqiang, Song, Xiaohong, Vaidya, Kedar R, Wang, Xilu, Wang, Jin, Xiao, Yu, Zhang, Haichao, Zhang, Xinxin, Blomme, Eric A, Boghaert, Erwin R, Kalvass, John C, Phillips, Andrew, Souers, Andrew J
Published in Science advances (04.10.2024)
Published in Science advances (04.10.2024)
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Journal Article
BCL-X L -targeting antibody-drug conjugates are active in preclinical models and mitigate on-mechanism toxicity of small-molecule inhibitors
Judd, Andrew S, Bawa, Bhupinder, Buck, Wayne R, Tao, Zhi-Fu, Li, Yingchun, Mitten, Michael J, Bruncko, Milan, Catron, Nathaniel, Doherty, George, Durbin, Kenneth R, Enright, Brian, Frey, Robin, Haasch, Deanna, Haman, Sandra, Haight, Anthony R, Henriques, Tracy A, Holms, James, Izeradjene, Kamel, Judge, Russell A, Jenkins, Gary J, Kunzer, Aaron, Leverson, Joel D, Martin, Ruth L, Mitra, Diya, Mittelstadt, Scott, Nelson, Lorne, Nimmer, Paul, Palma, Joann, Peterson, Richard, Phillips, Darren C, Ralston, Sherry L, Rosenberg, Saul H, Shen, Xiaoqiang, Song, Xiaohong, Vaidya, Kedar R, Wang, Xilu, Wang, Jin, Xiao, Yu, Zhang, Haichao, Zhang, Xinxin, Blomme, Eric A, Boghaert, Erwin R, Kalvass, John C, Phillips, Andrew, Souers, Andrew J
Published in Science advances (04.10.2024)
Published in Science advances (04.10.2024)
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Journal Article
Discovery of A‑1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL‑XL Inhibitor
Wang, Le, Doherty, George A, Judd, Andrew S, Tao, Zhi-Fu, Hansen, T. Matthew, Frey, Robin R, Song, Xiaohong, Bruncko, Milan, Kunzer, Aaron R, Wang, Xilu, Wendt, Michael D, Flygare, John A, Catron, Nathaniel D, Judge, Russell A, Park, Chang H, Shekhar, Shashank, Phillips, Darren C, Nimmer, Paul, Smith, Morey L, Tahir, Stephen K, Xiao, Yu, Xue, John, Zhang, Haichao, Le, Phuong N, Mitten, Michael J, Boghaert, Erwin R, Gao, Wenqing, Kovar, Peter, Choo, Edna F, Diaz, Dolores, Fairbrother, Wayne J, Elmore, Steven W, Sampath, Deepak, Leverson, Joel D, Souers, Andrew James
Published in ACS medicinal chemistry letters (08.10.2020)
Published in ACS medicinal chemistry letters (08.10.2020)
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Journal Article
Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents
King, Andrew J, Judd, Andrew S, Souers, Andrew J
Published in Expert opinion on therapeutic patents (01.01.2010)
Published in Expert opinion on therapeutic patents (01.01.2010)
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Journal Article
Identification of 2-(4-Benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an Orally Efficacious Melanin-Concentrating Hormone Receptor 1 Antagonist for the Treatment of Obesity
Souers, Andrew J, Gao, Ju, Brune, Michael, Bush, Eugene, Wodka, Dariusz, Vasudevan, Anil, Judd, Andrew S, Mulhern, Mathew, Brodjian, Sevan, Dayton, Brian, Shapiro, Robin, Hernandez, Lisa E, Marsh, Kennan C, Sham, Hing L, Collins, Christine A, Kym, Philip R
Published in Journal of medicinal chemistry (10.03.2005)
Published in Journal of medicinal chemistry (10.03.2005)
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Discovery and SAR development of thienopyridones: A class of small molecule AMPK activators
Zhao, Gang, Iyengar, Rajesh R., Judd, Andrew S., Cool, Barbara, Chiou, William, Kifle, Lemma, Frevert, Ernst, Sham, Hing, Kym, Philip R.
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
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ANTI-EGFR ANTIBODY DRUG CONJUGATE
ANDREW C PHILLIPS, ANDREW J SOUERS, ANDREW S JUDD, ERWIN R BOGHAERT, MILAN BRUNCKO
Year of Publication 21.11.2023
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Year of Publication 21.11.2023
Patent
Optimization of Chromone-2-carboxamide Melanin Concentrating Hormone Receptor 1 Antagonists: Assessment of Potency, Efficacy, and Cardiovascular Safety
Lynch, John K, Freeman, Jennifer C, Judd, Andrew S, Iyengar, Rajesh, Mulhern, Mathew, Zhao, Gang, Napier, James J, Wodka, Dariusz, Brodjian, Sevan, Dayton, Brian D, Falls, Doug, Ogiela, Christopher, Reilly, Regina M, Campbell, Thomas J, Polakowski, James S, Hernandez, Lisa, Marsh, Kennan C, Shapiro, Robin, Knourek-Segel, Victoria, Droz, Brian, Bush, Eugene, Brune, Michael, Preusser, Lee C, Fryer, Ryan M, Reinhart, Glenn A, Houseman, Kathryn, Diaz, Gilbert, Mikhail, Ann, Limberis, James T, Sham, Hing L, Collins, Christine A, Kym, Philip R
Published in Journal of medicinal chemistry (02.11.2006)
Published in Journal of medicinal chemistry (02.11.2006)
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Journal Article
Process Development of a Diacyl Glycerolacyltransferase-1 Inhibitor
Ravn, Matthew M, Wagaw, Seble H, Engstrom, Kenneth M, Mei, Jianzhang, Kotecki, Brian, Souers, Andrew J, Kym, Philip R, Judd, Andrew S, Zhao, Gang
Published in Organic process research & development (19.03.2010)
Published in Organic process research & development (19.03.2010)
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