Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex von Hao, Qi, Rathinaswamy, Manoj K., Klinge, Kelly L., Bratkowski, Matthew, Mafi, Amirhossein, Baumgartner, Christina K., Hamel, Keith M., Veits, Gesine K., Jain, Rinku, Catalano, Claudio, Fitzgerald, Mark, Hird, Alexander W., Park, Eunice, Vora, Harit U., Henderson, James A., Longenecker, Kenton, Hutchins, Charles W., Qiu, Wei, Scapin, Giovanna, Sun, Qi, Stoll, Vincent S., Sun, Chaohong, Li, Ping, Eaton, Dan, Stokoe, David, Fisher, Stewart L., Nasveschuk, Christopher G., Paddock, Marcia, Kort, Michael E.

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Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels von Chen, Jun, Zhang, Xu-Feng, Kort, Michael E, Huth, Jeffrey R, Sun, Chaohong, Miesbauer, Laura J, Cassar, Steven C, Neelands, Torben, Scott, Victoria E, Moreland, Robert B, Reilly, Regina M, Hajduk, Philip J, Kym, Philip R, Hutchins, Charles W, Faltynek, Connie R

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Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy von Szczepankiewicz, Bruce G, Liu, Gang, Hajduk, Philip J, Abad-Zapatero, Cele, Pei, Zhonghua, Xin, Zhili, Lubben, Thomas H, Trevillyan, James M, Stashko, Michael A, Ballaron, Stephen J, Liang, Heng, Huang, Flora, Hutchins, Charles W, Fesik, Stephen W, Jirousek, Michael R

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Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Beh... von Sheikh, Ahmad Y., Mattei, Alessandra, Miglani Bhardwaj, Rajni, Hong, Richard S., Abraham, Nathan S., Schneider-Rauber, Gabriela, Engstrom, Kenneth M., Diwan, Moiz, Henry, Rodger F., Gao, Yi, Juarez, Vivian, Jordan, Erin, DeGoey, David A., Hutchins, Charles W.

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Fragment Screening and Assembly:  A Highly Efficient Approach to a Selective and Cell Active Protein Tyrosine Phosphatase 1B Inhibitor von Liu, Gang, Xin, Zhili, Pei, Zhonghua, Hajduk, Philip J, Abad-Zapatero, Cele, Hutchins, Charles W, Zhao, Hongyu, Lubben, Thomas H, Ballaron, Stephen J, Haasch, Deanna L, Kaszubska, Wiweka, Rondinone, Cristina M, Trevillyan, James M, Jirousek, Michael R

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CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16 von Shergalis, Andrea G., Marin, Violeta L., Rhee, David Y., Senaweera, Sameera, McCloud, Rebecca L., Ronau, Judith A., Hutchins, Charles W., McLoughlin, Shaun, Woller, Kevin R., Warder, Scott E., Vasudevan, Anil, Reitsma, Justin M.

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Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Br... von McDaniel, Keith F, Wang, Le, Soltwedel, Todd, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Mantei, Robert A, Pratt, John K, Sheppard, George S, Bui, Mai H, Faivre, Emily J, Huang, Xiaoli, Li, Leiming, Lin, Xiaoyu, Wang, Rongqi, Warder, Scott E, Wilcox, Denise, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Park, Chang H, Hutchins, Charles W, Shen, Jianwei J, Edalji, Rohinton P, Sun, Chaohong C, Martin, Ruth, Gao, Wenqing, Wong, Shekman, Fang, Guowei, Elmore, Steven W, Shen, Yu, Kati, Warren M

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Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer’s Disease: 2‑(3-Phenyl‑1H‑pyrazol-1-yl)-nicotinamides von Kling, Andreas, Jantos, Katja, Mack, Helmut, Hornberger, Wilfried, Drescher, Karla, Nimmrich, Volker, Relo, Ana, Wicke, Karsten, Hutchins, Charles W, Lao, Yanbin, Marsh, Kennan, Moeller, Achim

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Current status and future prospects for enabling chemistry technology in the drug discovery process [version 1; peer review: 2 approved] von Djuric, Stevan W, Hutchins, Charles W, Talaty, Nari N

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Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo von Randolph, John T., O’Connor, Matthew J., Han, Fei, Hutchins, Charles W., Siu, Y. Amy, Cho, Min, Zheng, Yunan, Hickson, Jonathan A., Markley, Jana L., Manaves, Vlasios, Algire, Mikkel, Baker, Kenton A., Chapman, Alex M., Gopalakrishnan, Sujatha M., Panchal, Sanjay C., Foster-Duke, Kelly, Stolarik, DeAnne F., Kempf-Grote, Anita, Dammeier, Darby, Fossey, Stacey, Sun, Qi, Sun, Chaohong, Shen, Yu, Dart, Michael J., Kati, Warren M., Lai, Albert, Firestone, Ari J., Kort, Michael E.

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Ligand association rates to the inner-variable-domain of a dual-variable-domain immunoglobulin are significantly impacted by linker design von DiGiammarino, Enrico L., Harlan, John E., Walter, Karl A., Ladror, Uri S., Edalji, Rohinton P., Hutchins, Charles W., Lake, Marc R., Greischar, Amy J., Liu, Junjian, Ghayur, Tariq, Jakob, Clarissa G.

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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors von Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F

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Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists von Geneste, Hervé, Bhowmik, Swati, van Gaalen, Marcel M., Hornberger, Wilfried, Hutchins, Charles W., Netz, Astrid, Oost, Thorsten, Unger, Liliane

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Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds von Ramos, Ashley L., Goedken, Eric R., Frank, Kristine E., Argiriadi, Maria A., Bazzaz, Sana, Bian, Zhiguo, Brown, Jesse T. C., Centrella, Paolo A., Chen, Hui-Ju, Disch, Jeremy S., Donner, Pamela L., Duignan, David B., Gikunju, Diana, Greszler, Stephen N., Guié, Marie-Aude, Habeshian, Sevan, Hartl, Hajnalka E., Hein, Christopher D., Hutchins, Charles W., Jetson, Rachael, Keefe, Anthony D., Khan, Hasan, Li, Huan-Qiu, Olszewski, Allison, Ortiz Cardona, Benjamin J., Osuma, Augustine, Panchal, Sanjay C., Phelan, Ryan, Qiu, Wei, Shotwell, J. Brad, Shrestha, Anurupa, Srikumaran, Myron, Su, Zhi, Sun, Chaohong, Upadhyay, Anup K., Wood, Michael D., Wu, Haihong, Zhang, Ruijie, Zhang, Ying, Zhao, Gang, Zhu, Haizhong, Webster, Matthew P.

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Analgesic potential of TRPV1 antagonists von Kym, Philip R., Kort, Michael E., Hutchins, Charles W.

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors von Fidanze, Steven D., Liu, Dachun, Mantei, Robert A., Hasvold, Lisa A., Pratt, John K., Sheppard, George S., Wang, Le, Holms, James H., Dai, Yujia, Aguirre, Ana, Bogdan, Andrew, Dietrich, Justin D., Marjanovic, Jasmina, Park, Chang H., Hutchins, Charles W., Lin, Xiaoyu, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise, Li, Leiming, Wang, Rongqi, Kovar, Peter, Magoc, Terrance J., Rajaraman, Ganesh, Albert, Daniel H., Shen, Yu, Kati, Warren M., McDaniel, Keith F.

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Identification of a monoacid-Based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B von Xin, Zhili, Liu, Gang, Abad-Zapatero, Cele, Pei, Zhonghua, Szczepankiewicz, Bruce G., Li, Xiaofeng, Zhang, Tianyuan, Hutchins, Charles W., Hajduk, Philip J., Ballaron, Stephen J., Stashko, Michael A., Lubben, Thomas H., Trevillyan, James M., Jirousek, Michael R.

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Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity von Szczepankiewicz, Bruce G, Kosogof, Christi, Nelson, Lissa T. J, Liu, Gang, Liu, Bo, Zhao, Hongyu, Serby, Michael D, Xin, Zhili, Liu, Mei, Gum, Rebecca J, Haasch, Deanna L, Wang, Sanyi, Clampit, Jill E, Johnson, Eric F, Lubben, Thomas H, Stashko, Michael A, Olejniczak, Edward T, Sun, Chaohong, Dorwin, Sarah A, Haskins, Kristi, Abad-Zapatero, Cele, Fry, Elizabeth H, Hutchins, Charles W, Sham, Hing L, Rondinone, Cristina M, Trevillyan, James M

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Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8 von Judge, Russell A, Zhu, Haizhong, Upadhyay, Anup K, Bodelle, Pierre M, Hutchins, Charles W, Torrent, Maricel, Marin, Violeta L, Yu, Wenyu, Vedadi, Masoud, Li, Fengling, Brown, Peter J, Pappano, William N, Sun, Chaohong, Petros, Andrew M

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Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors von SIPPY, Kevin B, ANDERSON, David J, BUNNELLE, William H, HUTCHINS, Charles W, SCHRIMPF, Michael R

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