Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases
Gerstenberger, Brian S, Ambler, Catherine, Arnold, Eric P, Banker, Mary-Ellen, Brown, Matthew F, Clark, James D, Dermenci, Alpay, Dowty, Martin E, Fensome, Andrew, Fish, Susan, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, David W, Lin, Tsung H, Owen, Dafydd R, Saiah, Eddine, Sharma, Raman, Vajdos, Felix F, Xing, Li, Yang, Xiaojing, Yang, Xin, Wright, Stephen W
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Journal Article
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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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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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)
Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Journal Article
The use of plasma aldosterone and urinary sodium to potassium ratio as translatable quantitative biomarkers of mineralocorticoid receptor antagonism
Eudy, Rena J, Sahasrabudhe, Vaishali, Sweeney, Kevin, Tugnait, Meera, King-Ahmad, Amanda, Near, Kristen, Loria, Paula, Banker, Mary Ellen, Piotrowski, David W, Boustany-Kari, Carine M
Published in Journal of translational medicine (21.10.2011)
Published in Journal of translational medicine (21.10.2011)
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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
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-(1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841
Fensome, Andrew, Ambler, Catherine M., Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F., Chrencik, Jill, Clark, James D., Dowty, Martin E., Efremov, Ivan V., Flick, Andrew, Gerstenberger, Brian S., Gopalsamy, Ariamala, Hayward, Matthew M., Hegen, Martin, Hollingshead, Brett D., Jussif, Jason, Knafels, John D., Limburg, David C., Lin, David, Lin, Tsung H., Pierce, Betsy S., Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T., Telliez, Jean-Baptiste, Trujillo, John I., Vajdos, Felix F., Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
Vazquez, Michael L, Kaila, Neelu, Strohbach, Joseph W, Trzupek, John D, Brown, Matthew F, Flanagan, Mark E, Mitton-Fry, Mark J, Johnson, Timothy A, TenBrink, Ruth E, Arnold, Eric P, Basak, Arindrajit, Heasley, Steven E, Kwon, Soojin, Langille, Jonathan, Parikh, Mihir D, Griffin, Sarah H, Casavant, Jeffrey M, Duclos, Brian A, Fenwick, Ashley E, Harris, Thomas M, Han, Seungil, Caspers, Nicole, Dowty, Martin E, Yang, Xin, Banker, Mary Ellen, Hegen, Martin, Symanowicz, Peter T, Li, Li, Wang, Lu, Lin, Tsung H, Jussif, Jason, Clark, James D, Telliez, Jean-Baptiste, Robinson, Ralph P, Unwalla, Ray
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 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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Journal Article
ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling
Thorarensen, Atli, Banker, Mary Ellen, Fensome, Andrew, Telliez, Jean-Baptiste, Juba, Brian, Vincent, Fabien, Czerwinski, Robert M, Casimiro-Garcia, Agustin
Published in ACS chemical biology (18.07.2014)
Published in ACS chemical biology (18.07.2014)
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Journal Article
Identification of Morpholino‑2H‑pyrido[3,2‑b][1,4]oxazin-3(4H)‑ones as Nonsteroidal Mineralocorticoid Antagonists
Piotrowski, David W, Futatsugi, Kentaro, Casimiro-Garcia, Agustin, Wei, Liuqing, Sammons, Matthew F, Herr, Michael, Jiao, Wenhua, Lavergne, Sophie Y, Coffey, Steven B, Wright, Stephen W, Song, Kun, Loria, Paula M, Banker, Mary Ellen, Petersen, Donna N, Bauman, Jonathan
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Journal Article
Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide
Liu, Shenping, Desharnais, Joel, Sahasrabudhe, Parag V, Jin, Ping, Li, Wei, Oates, Bryan D, Shanker, Suman, Banker, Mary Ellen, Chrunyk, Boris A, Song, Xi, Feng, Xidong, Griffor, Matt, Jimenez, Judith, Chen, Gang, Tumelty, David, Bhat, Abhijit, Bradshaw, Curt W, Woodnutt, Gary, Lappe, Rodney W, Thorarensen, Atli, Qiu, Xiayang, Withka, Jane M, Wood, Lauren D
Published in Scientific reports (17.05.2016)
Published in Scientific reports (17.05.2016)
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Journal Article
Demonstration of In Vitro to In Vivo Translation of a TYK2 Inhibitor That Shows Cross Species Potency Differences
Gerstenberger, Brian S, Banker, Mary Ellen, Clark, James D, Dowty, Martin E, Fensome, Andrew, Gifford, Roger, Griffor, Matthew C, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, Tsung H, Smith, James F, Vajdos, Felix F
Published in Scientific reports (02.06.2020)
Published in Scientific reports (02.06.2020)
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Journal Article
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
Liu, Shenping, Dakin, Leslie A, Xing, Li, Withka, Jane M, Sahasrabudhe, Parag V, Li, Wei, Banker, Mary Ellen, Balbo, Paul, Shanker, Suman, Chrunyk, Boris A, Guo, Zuojun, Chen, Jinshan M, Young, Jennifer A, Bai, Guoyun, Starr, Jeremy T, Wright, Stephen W, Bussenius, Joerg, Tan, Sheng, Gopalsamy, Ariamala, Lefker, Bruce A, Vincent, Fabien, Jones, Lyn H, Xu, Hua, Hoth, Lise R, Geoghegan, Kieran F, Qiu, Xiayang, Bunnage, Mark E, Thorarensen, Atli
Published in Scientific reports (16.08.2016)
Published in Scientific reports (16.08.2016)
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Journal Article
Identification of Morpholino-2 H -pyrido[3,2- b ][1,4]oxazin-3(4 H )-ones as Nonsteroidal Mineralocorticoid Antagonists
Piotrowski, David W., Futatsugi, Kentaro, Casimiro-Garcia, Agustin, Wei, Liuqing, Sammons, Matthew F., Herr, Michael, Jiao, Wenhua, Lavergne, Sophie Y., Coffey, Steven B., Wright, Stephen W., Song, Kun, Loria, Paula M., Banker, Mary Ellen, Petersen, Donna N., Bauman, Jonathan
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Journal Article
Identification of (R)‑6-(1-(4-Cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro‑1H‑pyrazol-3-yl)-2-methoxynicotinic Acid, a Highly Potent and Selective Nonsteroidal Mineralocorticoid Receptor Antagonist
Casimiro-Garcia, Agustin, Piotrowski, David W, Ambler, Catherine, Arhancet, Graciela B, Banker, Mary Ellen, Banks, Tereece, Boustany-Kari, Carine M, Cai, Cuiman, Chen, Xiangyang, Eudy, Rena, Hepworth, David, Hulford, Catherine A, Jennings, Sandra M, Loria, Paula M, Meyers, Marvin J, Petersen, Donna N, Raheja, Neil K, Sammons, Matthew, She, Li, Song, Kun, Vrieze, Derek, Wei, Liuqing
Published in Journal of medicinal chemistry (22.05.2014)
Published in Journal of medicinal chemistry (22.05.2014)
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Journal Article
Identification of ( R )-6-(1-(4-Cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1 H -pyrazol-3-yl)-2-methoxynicotinic Acid, a Highly Potent and Selective Nonsteroidal Mineralocorticoid Receptor Antagonist
Casimiro-Garcia, Agustin, Piotrowski, David W., Ambler, Catherine, Arhancet, Graciela B., Banker, Mary Ellen, Banks, Tereece, Boustany-Kari, Carine M., Cai, Cuiman, Chen, Xiangyang, Eudy, Rena, Hepworth, David, Hulford, Catherine A., Jennings, Sandra M., Loria, Paula M., Meyers, Marvin J., Petersen, Donna N., Raheja, Neil K., Sammons, Matthew, She, Li, Song, Kun, Vrieze, Derek, Wei, Liuqing
Published in Journal of medicinal chemistry (22.05.2014)
Published in Journal of medicinal chemistry (22.05.2014)
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Journal Article
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)‑2,2-Difluorocyclopropyl)((1R,5S)‑3-(2-((1-methyl‑1H‑pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)
Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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