Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors
Casimiro-Garcia, Agustin, Trujillo, John I, Vajdos, Felix, Juba, Brian, Banker, Mary Ellen, Aulabaugh, Ann, Balbo, Paul, Bauman, Jonathan, Chrencik, Jill, Coe, Jotham W, Czerwinski, Robert, Dowty, Martin, Knafels, John D, Kwon, Soojin, Leung, Louis, Liang, Sidney, Robinson, Ralph P, Telliez, Jean-Baptiste, Unwalla, Ray, Yang, Xin, Thorarensen, Atli
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
Target the More Druggable Protein States in a Highly Dynamic Protein–Protein Interaction System
Guo, Zuojun, Thorarensen, Atli, Che, Jianwei, Xing, Li
Published in Journal of chemical information and modeling (25.01.2016)
Published in Journal of chemical information and modeling (25.01.2016)
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Journal Article
Implementation of combined approaches to quantify plasma protein binding of bRo5 compounds
Li, Na, Taylor, Simon, Davoren, Jennifer, Diner, Colin, Wang, Yi, Han, Chunyan, Jiao, Xingjin, Xu, Mandy, Thorarensen, Atli
Published in Drug metabolism and pharmacokinetics (01.04.2024)
Published in Drug metabolism and pharmacokinetics (01.04.2024)
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Journal Article
Structural basis for CCR6 modulation by allosteric antagonists
Wasilko, David Jonathan, Gerstenberger, Brian S, Farley, Kathleen A, Li, Wei, Alley, Jennifer, Schnute, Mark E, Unwalla, Ray J, Victorino, Jorge, Crouse, Kimberly K, Ding, Ru, Sahasrabudhe, Parag V, Vincent, Fabien, Frisbie, Richard K, Dermenci, Alpay, Flick, Andrew, Choi, Chulho, Chinigo, Gary, Mousseau, James J, Trujillo, John I, Nuhant, Philippe, Mondal, Prolay, Lombardo, Vincent, Lamb, Daniel, Hogan, Barbara J, Minhas, Gurdeep Singh, Segala, Elena, Oswald, Christine, Windsor, Ian W, Han, Seungil, Rappas, Mathieu, Cooke, Robert M, Calabrese, Matthew F, Berstein, Gabriel, Thorarensen, Atli, Wu, Huixian
Published in Nature communications (31.08.2024)
Published in Nature communications (31.08.2024)
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Journal Article
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5-((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli, Dowty, Martin E, Banker, Mary Ellen, Juba, Brian, Jussif, Jason, Lin, Tsung, Vincent, Fabien, Czerwinski, Robert M, Casimiro-Garcia, Agustin, Unwalla, Ray, Trujillo, John I, Liang, Sidney, Balbo, Paul, Che, Ye, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Leung, Louis, Yang, Xin, Soucy, Sarah, Hegen, Martin, Coe, Jotham, Langille, Jonathan, Vajdos, Felix, Chrencik, Jill, Telliez, Jean-Baptiste
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
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Journal Article
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation
Gierse, James, Thorarensen, Atli, Beltey, Konstantine, Bradshaw-Pierce, Erica, Cortes-Burgos, Luz, Hall, Troii, Johnston, Amy, Murphy, Michael, Nemirovskiy, Olga, Ogawa, Shinji, Pegg, Lyle, Pelc, Matthew, Prinsen, Michael, Schnute, Mark, Wendling, Jay, Wene, Steve, Weinberg, Robin, Wittwer, Arthur, Zweifel, Ben, Masferrer, Jaime
Published in The Journal of pharmacology and experimental therapeutics (01.07.2010)
Published in The Journal of pharmacology and experimental therapeutics (01.07.2010)
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Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters
Trujillo, John I., Kiefer, James R., Huang, Wei, Day, Jacqueline E., Moon, Joseph, Jerome, Gina M., Bono, Christine P., Kornmeier, Christine M., Williams, Melanie L., Kuhn, Cyrille, Rennie, Glen R., Wynn, Thomas A., Carron, Christopher P., Thorarensen, Atli
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 11. The Synthesis of (+)-Crotanecine
Denmark, Scott E, Thorarensen, Atli
Published in Journal of the American Chemical Society (08.01.1997)
Published in Journal of the American Chemical Society (08.01.1997)
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Journal Article
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS)
Carron, Chris P, Trujillo, John I, Olson, Kirk L, Huang, Wei, Hamper, Bruce C, Dice, Tom, Neal, Bradley E, Pelc, Matthew J, Day, Jacqueline E, Rohrer, Douglas C, Kiefer, James R, Moon, Joseph B, Schweitzer, Barbara A, Blake, Tanisha D, Turner, Steve R, Woerndle, Rhonda, Case, Brenda L, Bono, Christine P, Dilworth, Vickie M, Funckes-Shippy, Christie L, Hood, Becky L, Jerome, Gina M, Kornmeier, Christine M, Radabaugh, Melissa R, Williams, Melanie L, Davies, Michael S, Wegner, Craig D, Welsch, Dean J, Abraham, William M, Warren, Chad J, Dowty, Martin E, Hua, Fengmei, Zutshi, Anup, Yang, Jerry Z, Thorarensen, Atli
Published in ACS medicinal chemistry letters (13.05.2010)
Published in ACS medicinal chemistry letters (13.05.2010)
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Journal Article
Chiral Benzoquinones as a New Class of Ligands for Asymmetric Catalysis: Synthesis and Application to the Palladium(II)-Catalyzed 1,4-Dialkoxylation of 1,3-Dienes
Itami, Kenichiro, Palmgren, Andreas, Thorarensen, Atli, Bäckvall, Jan-E
Published in Journal of organic chemistry (18.09.1998)
Published in Journal of organic chemistry (18.09.1998)
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Journal Article
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-(2s,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-y1)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli, Dowty, Martin E., Banker, Mary Ellen, Juba, Brian, Jussif, Jason, Lin, Tsung, Vincent, Fabien, Czerwinski, Robert M., Casimiro-Garcia, Agustin, Unwalla, Ray, Trujillo, John I., Liang, Sidney, Balbo, Paul, Che, Ye, Gilbert, Adam M., Brown, Matthew F., Hayward, Matthew, Montgomery, Justin, Leung, Louis, Yang, Xin, Soucy, Sarah, Hegen, Martin, Coe, Jotham, Langille, Jonathan, Vajdos, Felix, Chrencik, Jill, Telliez, Jean-Baptiste
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
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Journal Article
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization
Thorarensen, Atli, Balbo, Paul, Banker, Mary E., Czerwinski, Robert M., Kuhn, Max, Maurer, Tristan S., Telliez, Jean-Baptiste, Vincent, Fabien, Wittwer, Arthur J.
Published in Bioorganic & medicinal chemistry (01.01.2021)
Published in Bioorganic & medicinal chemistry (01.01.2021)
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Journal Article
PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor
Xu, Hua, Jesson, Michael I, Seneviratne, Uthpala I, Lin, Tsung H, Sharif, M. Nusrat, Xue, Liang, Nguyen, Chuong, Everley, Robert A, Trujillo, John I, Johnson, Douglas S, Point, Gary R, Thorarensen, Atli, Kilty, Iain, Telliez, Jean-Baptiste
Published in ACS chemical biology (21.06.2019)
Published in ACS chemical biology (21.06.2019)
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Journal Article
From in silico to in Vitro to In Vivo : Increasing Megakaryocytes to Treat Thrombocytopenia
Macias, Alejandra, Cortes, Mauricio, An, Na, Li, Na, Fulton, Timothy, Simpson, Allison, Miller, Samuel, Sun, Sunny, Fu, Doris, Garcia, Juan, Medicherla, Satya, Steelman, Scott, Thorarensen, Atli, Goddeeris, Matthew, Krishnamoorthy, Sriram
Published in Blood (02.11.2023)
Published in Blood (02.11.2023)
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Journal Article
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition
Telliez, Jean-Baptiste, Dowty, Martin E, Wang, Lu, Jussif, Jason, Lin, Tsung, Li, Li, Moy, Erick, Balbo, Paul, Li, Wei, Zhao, Yajuan, Crouse, Kimberly, Dickinson, Caitlyn, Symanowicz, Peter, Hegen, Martin, Banker, Mary Ellen, Vincent, Fabien, Unwalla, Ray, Liang, Sidney, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Yang, Xin, Bauman, Jonathan, Trujillo, John I, Casimiro-Garcia, Agustin, Vajdos, Felix F, Leung, Louis, Geoghegan, Kieran F, Quazi, Amira, Xuan, Dejun, Jones, Lyn, Hett, Erik, Wright, Katherine, Clark, James D, Thorarensen, Atli
Published in ACS chemical biology (16.12.2016)
Published in ACS chemical biology (16.12.2016)
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