Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition
Boudreau, Aaron, Purkey, Hans E, Hitz, Anna, Robarge, Kirk, Peterson, David, Labadie, Sharada, Kwong, Mandy, Hong, Rebecca, Gao, Min, Del Nagro, Christopher, Pusapati, Raju, Ma, Shuguang, Salphati, Laurent, Pang, Jodie, Zhou, Aihe, Lai, Tommy, Li, Yingjie, Chen, Zhongguo, Wei, Binqing, Yen, Ivana, Sideris, Steve, McCleland, Mark, Firestein, Ron, Corson, Laura, Vanderbilt, Alex, Williams, Simon, Daemen, Anneleen, Belvin, Marcia, Eigenbrot, Charles, Jackson, Peter K, Malek, Shiva, Hatzivassiliou, Georgia, Sampath, Deepak, Evangelista, Marie, O'Brien, Thomas
Published in Nature chemical biology (01.10.2016)
Published in Nature chemical biology (01.10.2016)
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A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors
Sohn, Sue J, Barrett, Kathy, Van Abbema, Anne, Chang, Christine, Kohli, Pawan Bir, Kanda, Hidenobu, Smith, Janice, Lai, Yingjie, Zhou, Aihe, Zhang, Birong, Yang, Wenqian, Williams, Karen, Macleod, Calum, Hurley, Christopher A, Kulagowski, Janusz J, Lewin-Koh, Nicholas, Dengler, Hart S, Johnson, Adam R, Ghilardi, Nico, Zak, Mark, Liang, Jun, Blair, Wade S, Magnuson, Steven, Wu, Lawren C
Published in The Journal of immunology (1950) (01.09.2013)
Published in The Journal of immunology (1950) (01.09.2013)
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Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists
Fauber, Benjamin P., Gobbi, Alberto, Robarge, Kirk, Zhou, Aihe, Barnard, Adrian, Cao, Jianhua, Deng, Yuzhong, Eidenschenk, Céline, Everett, Christine, Ganguli, Arunima, Hawkins, Julie, Johnson, Adam R., La, Hank, Norman, Maxine, Salmon, Gary, Summerhill, Susan, Ouyang, Wenjun, Tang, Wei, Wong, Harvey
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Hanan, Emily J, van Abbema, Anne, Barrett, Kathy, Blair, Wade S, Blaney, Jeff, Chang, Christine, Eigenbrot, Charles, Flynn, Sean, Gibbons, Paul, Hurley, Christopher A, Kenny, Jane R, Kulagowski, Janusz, Lee, Leslie, Magnuson, Steven R, Morris, Claire, Murray, Jeremy, Pastor, Richard M, Rawson, Tom, Siu, Michael, Ultsch, Mark, Zhou, Aihe, Sampath, Deepak, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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A Pentacyclic Aurora Kinase Inhibitor (AKI-001) with High in Vivo Potency and Oral Bioavailability
Rawson, Thomas E, Rüth, Matthias, Blackwood, Elizabeth, Burdick, Dan, Corson, Laura, Dotson, Jenna, Drummond, Jason, Fields, Carter, Georges, Guy J, Goller, Bernhard, Halladay, Jason, Hunsaker, Thomas, Kleinheinz, Tracy, Krell, Hans-Willi, Li, Jun, Liang, Jun, Limberg, Anja, McNutt, Angela, Moffat, John, Phillips, Gail, Ran, Yingqing, Safina, Brian, Ultsch, Mark, Walker, Leslie, Wiesmann, Christian, Zhang, Birong, Zhou, Aihe, Zhu, Bing-Yan, Rüger, Petra, Cochran, Andrea G
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Journal Article
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Wei, BinQing, Robarge, Kirk, Labadie, Sharada S., Chen, Jinhua, Corson, Laura B., DiPasquale, Antonio, Dragovich, Peter S., Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P., Hitz, Anna, Hong, Rebecca, Lai, Kwong Wah, Liu, Wenfeng, Ma, Shuguang, Malek, Shiva, O'Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steven, Ultsch, Mark, Xu, Zijin, Yen, Ivana, Yu, Dong, Yue, Qin, Zhou, Aihe, Purkey, Hans E.
Published in Bioorganic & medicinal chemistry letters (19.01.2022)
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Published in Bioorganic & medicinal chemistry letters (19.01.2022)
Journal Article
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Wei, BinQing, Robarge, Kirk, Labadie, Sharada S., Chen, Jinhua, Corson, Laura B., DiPasquale, Antonio, Dragovich, Peter S., Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P., Hitz, Anna, Hong, Rebecca, Lai, Kwong Wah, Liu, Wenfeng, Ma, Shuguang, Malek, Shiva, O'Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sampath, Deepak, Sideris, Steven, Ultsch, Mark, Xu, Zijin, Yen, Ivana, Yu, Dong, Yue, Qin, Zhou, Aihe, Purkey, Hans E.
Published in Bioorganic & medicinal chemistry letters (01.03.2022)
Published in Bioorganic & medicinal chemistry letters (01.03.2022)
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Journal Article
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
Purkey, Hans E, Robarge, Kirk, Chen, Jinhua, Chen, Zhongguo, Corson, Laura B, Ding, Charles Z, DiPasquale, Antonio G, Dragovich, Peter S, Eigenbrot, Charles, Evangelista, Marie, Fauber, Benjamin P, Gao, Zhenting, Ge, Hongxiu, Hitz, Anna, Ho, Qunh, Labadie, Sharada S, Lai, Kwong Wah, Liu, Wenfeng, Liu, Yajing, Li, Chiho, Ma, Shuguang, Malek, Shiva, O’Brien, Thomas, Pang, Jodie, Peterson, David, Salphati, Laurent, Sideris, Steve, Ultsch, Mark, Wei, BinQing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhou, Aihe
Published in ACS medicinal chemistry letters (13.10.2016)
Published in ACS medicinal chemistry letters (13.10.2016)
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Journal Article
Discovery of (S)‑1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl‑1H‑pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)‑one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development
Blake, James F, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Dudley, Danette A, Gaudino, John J, Gould, Stephen E, Grina, Jonas, Hunsaker, Thomas, Liu, Lichuan, Martinson, Matthew, Moreno, David, Mueller, Lars, Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Robarge, Kirk, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Jianping, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John, Schwarz, Jacob B
Published in Journal of medicinal chemistry (23.06.2016)
Published in Journal of medicinal chemistry (23.06.2016)
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Journal Article
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase
Dragovich, Peter S., Fauber, Benjamin P., Boggs, Jason, Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Li, Chiho, Liu, Yichin, Liu, Yingchun, Ma, Shuguang, Malek, Shiva, Peterson, David, Pitts, Keith E., Purkey, Hans E., Robarge, Kirk, Salphati, Laurent, Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wang, Jing, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying, Zhou, Aihe
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
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Journal Article
Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase
Fauber, Benjamin P., Dragovich, Peter S., Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Labadie, Sharada, Malek, Shiva, Peterson, David, Purkey, Hans E., Robarge, Kirk, Sideris, Steve, Ultsch, Mark, Wei, BinQing, Yen, Ivana, Yue, Qin, Zhou, Aihe
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
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Journal Article
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase
Labadie, Sharada, Dragovich, Peter S., Chen, Jinhua, Fauber, Benjamin P., Boggs, Jason, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Ho, Qunh, Lai, Kwong Wah, Ma, Shuguang, Malek, Shiva, Peterson, David, Purkey, Hans E., Robarge, Kirk, Salphati, Laurent, Sideris, Steven, Ultsch, Mark, VanderPorten, Erica, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying, Zhou, Aihe
Published in Bioorganic & medicinal chemistry letters (01.01.2015)
Published in Bioorganic & medicinal chemistry letters (01.01.2015)
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A pentacyclic aurora kinase inhihitor (AKI-001) with high in vivo potency and oral bioavailability
Rawson, Thomas E., Rueth, Matthias, Blackwood, Elizabeth, Burdick, Dan, Corson, Laura, Dotson, Jenna, Drummond, Jason, Fields, Carter, Georges, Guy J., Goller, Bernhard, Halladay, Jason, Hunsaker, Thomas, Kleinheinz, Tracy, Krell, Hans-Willi, Li, Jun, Liang, Jun, Limberg, Anja, McNutt, Angela, Moffat, John, Phillips, Gail, Ran, Yingqing, Safina, Brian, Ultsch, Mark, Walker, Leslie, Wiesmann, Christian, Zhang, Birong, Zhou, Aihe, Zhu, Bing-Yan, Rueger, Petra, Cochran, Andrea G.
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Journal Article
Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development
Robarge, Kirk, Schwarz, Jacob, Blake, Jim, Burkard, Michael, Chan, Jocelyn, Chen, Huifen, Chou, Kang-Jye, Diaz, Dolores, Gaudino, John, Gould, Stephen, Grina, Jonas, Linghu, Xin, Liu, Lichuan, Martinson, Matthew, Moreno, David A., Orr, Christine, Pacheco, Patricia, Qin, Ann, Rasor, Kevin, Ren, Li, Shahidi-Latham, Sheerin, Stults, Jeffrey, Sullivan, Francis, Wang, Weiru, Yin, Peter, Zhou, Aihe, Belvin, Marcia, Merchant, Mark, Moffat, John G.
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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STEVEN R MAGNUSON, RICHARD PASTOR, THOMAS E RAWSON, ZHU BING-YAN, JOSEPH P LYSSIKATOS, EMILY HANAN, MICHAEL SIU, PAUL GIBBONS, ROHAN MENDONCA, WENDY LIU, MARK E ZAK, ZHOU AIHE
Year of Publication 07.11.2019
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Year of Publication 07.11.2019
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CHAN BRYAN, WEI BINQING, LU AIJUN, WANG WEIRU, CARTWRIGHT MATTHEW W, LIANG JUN, HEFFRON TIMOTHY, FAVOR DAVID, DANIELS BLAKE, MADIN ANDREW, HU YONGHAN, MALHOTRA SUSHANT, ZHOU AIHE, GOOD ANDREW, TELLIS JOHN, DROBNICK JOY, SEWARD EILEEN, LAINCHBURY MICHAEL, HUESTIS MALCOLM, JONES GRAHAM, FONG KIN CHIU, SIU MICHAEL, RAJAPAKSA NAOMI, HU BAIHUA, GANCIA EMANUELA, MENDONCA ROHAN, STIVALA CRAIG, GAZZARD LEWIS
Year of Publication 09.12.2019
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Year of Publication 09.12.2019
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HPK1의 억제제인 이소퀴놀린
GOOD ANDREW, TELLIS JOHN, CHAN BRYAN, DROBNICK JOY, WEI BINQING, WANG WEIRU, SEWARD EILEEN, LAINCHBURY MICHAEL, CARTWRIGHT MATTHEW W, LIANG JUN, FONG KIN CHIU, HEFFRON TIMOTHY, FAVOR DAVID, RAJAPAKSA NAOMI, GANCIA EMANUELA, MENDONCA ROHAN, MADIN ANDREW, HU YONGHAN, MALHOTRA SUSHANT, STIVALA CRAIG, ZHOU AIHE, GAZZARD LEWIS
Year of Publication 05.12.2019
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Year of Publication 05.12.2019
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