Structural basis for dual-mode inhibition of the ABC transporter MsbA von Ho, Hoangdung, Miu, Anh, Alexander, Mary Kate, Garcia, Natalie K., Oh, Angela, Zilberleyb, Inna, Reichelt, Mike, Austin, Cary D., Tam, Christine, Shriver, Stephanie, Hu, Huiyong, Labadie, Sharada S., Liang, Jun, Wang, Lan, Wang, Jian, Lu, Yan, Purkey, Hans E., Quinn, John, Franke, Yvonne, Clark, Kevin, Beresini, Maureen H., Tan, Man-Wah, Sellers, Benjamin D., Maurer, Till, Koehler, Michael F. T., Wecksler, Aaron T., Kiefer, James R., Verma, Vishal, Xu, Yiming, Nishiyama, Mireille, Payandeh, Jian, Koth, Christopher M.

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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer von Liang, Jun, Zbieg, Jason R., Blake, Robert A., Chang, Jae H., Daly, Stephen, DiPasquale, Antonio G., Friedman, Lori S., Gelzleichter, Thomas, Gill, Matthew, Giltnane, Jennifer M., Goodacre, Simon, Guan, Jane, Hartman, Steven J., Ingalla, Ellen Rei, Kategaya, Lorn, Kiefer, James R., Kleinheinz, Tracy, Labadie, Sharada S., Lai, Tommy, Li, Jun, Liao, Jiangpeng, Liu, Zhiguo, Mody, Vidhi, McLean, Neville, Metcalfe, Ciara, Nannini, Michelle A., Oeh, Jason, O’Rourke, Martin G., Ortwine, Daniel F., Ran, Yingqing, Ray, Nicholas C., Roussel, Fabien, Sambrone, Amy, Sampath, Deepak, Schutt, Leah K., Vinogradova, Maia, Wai, John, Wang, Tao, Wertz, Ingrid E., White, Jonathan R., Yeap, Siew Kuen, Young, Amy, Zhang, Birong, Zheng, Xiaoping, Zhou, Wei, Zhong, Yu, Wang, Xiaojing

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Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition von 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

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Enyne Amides to Fused Pyridones: Scope and Limitations von Labadie, Sharada S., Thai, Karine, Grandner, Jessica M., Liu, Yanzhou, Parr, Brendan T.

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Discovery of Inhibitors of the Lipopolysaccharide Transporter MsbA: From a Screening Hit to Potent Wild-Type Gram-Negative Activity von Verma, Vishal A, Wang, Lan, Labadie, Sharada S, Liang, Jun, Sellers, Benjamin D, Wang, Jian, Dong, Liting, Wang, Qiuyue, Zhang, Shuang, Xu, Zhongya, Zhang, Yexia, Niu, Yanan, Wang, Xinxin, Wai, John, Koehler, Michael F. T, Hu, Huiyong, Alexander, Mary Kate, Nishiyama, Mireille, Miu, Anh, Xu, Yiming, Pang, Jodie, Katakam, Anand K, Reichelt, Michael, Austin, Cary D, Ho, Hoangdung, Payandeh, Jian, Koth, Christopher M

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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase von 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.

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Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927 von Labadie, Sharada S., Li, Jun, Blake, Robert A., Chang, Jae H., Goodacre, Simon, Hartman, Steven J., Liang, Weiling, Kiefer, James R., Kleinheinz, Tracy, Lai, Tommy, Liao, Jiangpeng, Ortwine, Daniel F., Mody, Vidhi, Ray, Nicholas C., Roussel, Fabien, Vinogradova, Maia, Yeap, Siew Kuen, Zhang, Birong, Zheng, Xiaoping, Zbieg, Jason R., Liang, Jun, Wang, Xiaojing

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Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase von Dragovich, Peter S., Fauber, Benjamin P., Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Ge, HongXiu, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Malek, Shiva, Pan, Borlan, Peterson, David, Pitts, Keith, Purkey, Hans E., Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wei, BinQing, Xu, Qing, Yen, Ivana, Yue, Qin, Zhang, Huihui, Zhang, Xuying

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Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase von Fauber, Benjamin P., Dragovich, Peter S., Chen, Jinhua, Corson, Laura B., Ding, Charles Z., Eigenbrot, Charles, Giannetti, Anthony M., Hunsaker, Thomas, Labadie, Sharada, Liu, Yichin, Liu, Yingchun, Malek, Shiva, Peterson, David, Pitts, Keith, Sideris, Steve, Ultsch, Mark, VanderPorten, Erica, Wang, Jing, Wei, BinQing, Yen, Ivana, Yue, Qin

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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies von Liang, Jun, Zhang, Birong, Labadie, Sharada, Ortwine, Daniel F., Vinogradova, Maia, Kiefer, James R., Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley

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Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors von Labadie, Sharada S., Dragovich, Peter S., Cummings, Richard T., Deshmukh, Gauri, Gustafson, Amy, Han, Ning, Harmange, Jean-Christophe, Kiefer, James R., Li, Yue, Liang, Jun, Liederer, Bianca M., Liu, Yichin, Manieri, Wanda, Mao, Wiefeng, Murray, Lesley, Ortwine, Daniel F., Trojer, Patrick, VanderPorten, Erica, Vinogradova, Maia, Wen, Li

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Discovery of N‑[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo‑1H‑pyridin-3-yl)-3-quinolyl]phenyl]­methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polym... von Talamas, Francisco X., Abbot, Sarah C., Anand, Shalini, Brameld, Ken A., Carter, David S., Chen, Jun, Davis, Dana, de Vicente, Javier, Fung, Amy D., Gong, Leyi, Harris, Seth F., Inbar, Petra, Labadie, Sharada S., Lee, Eun K., Lemoine, Remy, Le Pogam, Sophie, Leveque, Vincent, Li, Jim, McIntosh, Joel, Nájera, Isabel, Park, Jaehyeon, Railkar, Aruna, Rajyaguru, Sonal, Sangi, Michael, Schoenfeld, Ryan C., Staben, Leanna R., Tan, Yunchou, Taygerly, Joshua P., Villaseñor, Armando G., Weller, Paul E.

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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice von 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

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De Novo Fragment Design: A Medicinal Chemistry Approach to Fragment-Based Lead Generation von Talamas, Francisco X, Ao-Ieong, Gloria, Brameld, Ken A, Chin, Elbert, de Vicente, Javier, Dunn, James P, Ghate, Manjiri, Giannetti, Anthony M, Harris, Seth F, Labadie, Sharada S, Leveque, Vincent, Li, Jim, Lui, Alfred S-T, McCaleb, Kristen L, Nájera, Isabel, Schoenfeld, Ryan C, Wang, Beihan, Wong, April

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Discovery of S-[5-Amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an Orally Bioavailable and Highly Selective Inhibitor of p38 Map... von Goldstein, David M, Alfredson, Tom, Bertrand, Jay, Browner, Michelle F, Clifford, Ken, Dalrymple, Stacie A, Dunn, James, Freire-Moar, Jose, Harris, Seth, Labadie, Sharada S, La Fargue, JoAnn, Lapierre, Jean Marc, Larrabee, Susan, Li, Fujun, Papp, Eva, McWeeney, Daniel, Ramesha, Chakk, Roberts, Rick, Rotstein, David, San Pablo, Bong, Sjogren, Eric B, So, On-Yee, Talamas, Francisco X, Tao, Will, Trejo, Alejandra, Villasenor, Armando, Welch, Mary, Welch, Teresa, Weller, Paul, Whiteley, Phyllis E, Young, Kelly, Zipfel, Sheila

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A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit von Cushing, Timothy D., Baichwal, Vijay, Berry, Karen, Billedeau, Roland, Bordunov, Viola, Broka, Chris, Cardozo, Mario, Cheng, Peng, Clark, David, Dalrymple, Stacie, DeGraffenreid, Michael, Gill, Adrian, Hao, Xiaolin, Hawley, Ronald C., He, Xiao, Jaen, Juan C., Labadie, Sharada S., Labelle, Marc, Lehel, Csaba, Lu, Pu-Ping, McIntosh, Joel, Miao, Shichang, Parast, Camran, Shin, Youngsook, Sjogren, Eric B., Smith, Marie-Louise, Talamas, Francisco X., Tonn, George, Walker, Keith M., Walker, Nigel P.C., Wesche, Holger, Whitehead, Chris, Wright, Matt, Browner, Michelle F.

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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER plus Breast Cancer von Liang, Jun, Zbieg, Jason R., Blake, Robert A., Chang, Jae H., Daly, Stephen, DiPasquale, Antonio G., Friedman, Lori S., Gelzleichter, Thomas, Gill, Matthew, Giltnane, Jennifer M., Goodacre, Simon, Guan, Jane, Hartman, Steven J., Ingalla, Ellen Rei, Kategaya, Lorn, Kiefer, James R., Kleinheinz, Tracy, Labadie, Sharada S., Lai, Tommy, Li, Jun, Liao, Jiangpeng, Liu, Zhiguo, Mody, Vidhi, McLean, Neville, Metcalfe, Ciara, Nannini, Michelle A., Oeh, Jason, O'Rourke, Martin G., Ortwine, Daniel F., Ran, Yingqing, Ray, Nicholas C., Roussel, Fabien, Sambrone, Amy, Sampath, Deepak, Schutt, Leah K., Vinogradova, Maia, Wai, John, Wang, Tao, Wertz, Ingrid E., White, Jonathan R., Yeap, Siew Kuen, Young, Amy, Zhang, Birong, Zheng, Xiaoping, Zhou, Wei, Zhong, Yu, Wang, Xiaojing

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A novel series of IKKβ inhibitors part II: Description of a potent and pharmacologically active series of analogs von Cushing, Timothy D., Baichwal, Vijay, Berry, Karen, Billedeau, Roland, Bordunov, Viola, Broka, Chris, Browner, Michelle F., Cardozo, Mario, Cheng, Peng, Clark, David, Dalrymple, Stacie, DeGraffenreid, Michael, Gill, Adrian, Hao, Xiaolin, Hawley, Ronald C., He, Xiao, Labadie, Sharada S., Labelle, Marc, Lehel, Csaba, Lu, Pu-Ping, McIntosh, Joel, Miao, Shichang, Parast, Camran, Shin, Youngsook, Sjogren, Eric B., Smith, Marie-Louise, Talamas, Francisco X., Tonn, George, Walker, Keith M., Walker, Nigel P.C., Wesche, Holger, Whitehead, Chris, Wright, Matt, Jaen, Juan C.

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Disrupting Gram-Negative Bacterial Outer Membrane Biosynthesis through Inhibition of the Lipopolysaccharide Transporter MsbA von Alexander, Mary Kate, Miu, Anh, Oh, Angela, Reichelt, Mike, Ho, Hoangdung, Chalouni, Cecile, Labadie, Sharada, Wang, Lan, Liang, Jun, Nickerson, Nicholas N, Hu, Huiyong, Yu, Lan, Du, Miaofen, Yan, Donghong, Park, Summer, Kim, Janice, Xu, Min, Sellers, Benjamin D, Purkey, Hans E, Skelton, Nicholas J, Koehler, Michael F T, Payandeh, Jian, Verma, Vishal, Xu, Yiming, Koth, Christopher M, Nishiyama, Mireille

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Indol-2-yltributylstannane: A Versatile Reagent for 2-Substituted Indoles von Labadie, Sharada S, Teng, Edmond

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