未登录Discovery of INCB126503 as a Potent and Selective FGFR2/3 InhibitorINCB126503作为强效且选择性FGFR2/3抑制剂的发现
Nguyen, MH; Wang, AL; Truong, L; Zhang, K; Ye, HF; Zhao, P; Horsey, A; Frascella, M; Leffet, L; Federowicz, K; Behshad, E; Witten, MR; Qi, C; Xu, Y; Jalluri, R; Harris, JJ; Hess, R; Sayers, B; Lin, LP; Yeleswaram, S; Zhang, GF; Kim, S; Covington, M; Diamond, S; Yao, WQ; Vechorkin, O .png)
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收藏Discovery of INCB159020, an Orally Bioavailable KRAS G12D Inhibitor发现INCB159020，一种口服生物利用的KRAS G12D抑制剂Ye, Qinda; Shvartsbart, Artem; Li, Zhenwu; Gan, Pei; Policarpo, Rocco L.; Qi, Chao; Roach, Jeremy J.; Zhu, Wenyu; Mccammant, Matthew S.; Hu, Bin; Li, Gencheng; Yin, Haolin; Carlsen, Peter; Hoang, Gia; Zhao, Le; Susick, Robert; Zhang, Fenglei; Lai, Cheng-Tsung; Hassani, Abdellah Allali; Epling, Leslie B.; Gallion, Alexandra; Kurzeja-Lipinski, Kerri; Gallagher, Karen; Roman, Valerie; Farren, Matthew R.; Kong, Weixi; Deller, Marc C.; Zhang, Guofeng; Covington, Maryanne; Diamond, Sharon; Kim, Sunkyu; Yao, Wenqing; Sokolsky, Alexander; Wang, Xiaozhao 分享 收藏 INCB161734: A novel, potent, and orally bioavailable KRAS G12D selective inhibitor demonstrates antitumor activity in KRAS G12D mutant tumorsFarren, Matthew R.; Roman, Valerie; Gallion, Alexandra; Allali-Hassani, Abdellah; Sokolsky, Alexander; Kong, Weixi; Smith, Amanda; Wang, Hui; Correa, Gina; Deller, Marc; Epling, Leslie B.; Procak, Jessica; Zhang, Guofeng; Pecko, Katherine; Kennedy, Keith; Boer, Jason; Kurzeja-Lipinski, Kerri; Covington, Maryanne; Chen, Kwang-Jong; Wallower, Renee; Rocha, Jennifer; Pan, Rina; Perry, Anthony; Yuska, Brad; Wang, Xiaozhao; Macarron, Ricardo; Kim, Sunkyu 分享 收藏 Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2Hummel, Joshua R.; Xiao, Kai-Jiong; Yang, Jeffrey C.; Epling, Leslie B.; Mukai Ken; Ye, Qinda; Xu, Meizhong; Qian, Dingquan; Huo, Lu; Weber, Michael; Roman, Valerie; Lo, Yvonne; Drake, Katherine; Stump, Kristine; Covington, Maryanne; Kapilashrami, Kanishk; Zhang, Guofeng; Ye, Min; Diamond, Sharon; Yeleswaram, Swamy; Macarron, Ricardo; Deller, Marc C.; Wee, Susan; Kim, Sunkyu; Wang, Xiaozhao; Wu, Liangxing; Yao, Wenqing 分享 收藏 Discovery of INCB098377: a potent inhibitor of phosphoinositide 3-kinase gamma (PI3Kγ)Arias, Diana A.; Douglass, Stephen; Truong, Lisa; Wang, Qian; Wang, Kathy H.; Yang, Gengjie; Hansbury, Michael; O'Connor, Sybil; Bowman, Kevin; Collins, Robert; Stubbs, Matthew; Hall, Leslie; Stevens, Christina; Maddage, Christopher; Douty, Brent; Covington, Maryanne; Leffet, Lynn; Yue, Eddy; Combs, Andrew; Kim, Sunkyu; Shin, Niu; Koblish, Holly; Hess, Rodrigo 分享 收藏 Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing ApproachNguyen, Minh H.; Ye, Hai -Fen; Xu, Yao; Truong, Lisa; Horsey, April; Zhao, Peng; Styduhar, Evan D.; Frascella, Michelle; Leffet, Lynn; Federowicz, Kelly; Behshad, Elham; Wang, Anlai; Zhang, Ke; Witten, Michael R.; Qi, Chao; Jalluri, Ravi; Lai, Cheng-Tsung; Atasoylu, Onur; Harris, Jennifer J.; Hess, Rodrigo; Lin, Luping; Zhang, Guofeng; Covington, Maryanne; Diamond, Sharon; Yao, Wenqing; Vechorkin, Oleg 分享 收藏 Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)Sokolsky, Alexander; Vechorkin, Oleg; Hummel, Joshua R.; Styduhar, Evan D.; Wang, Anlai; Nguyen, Minh H.; Ye, Hai Fen; Liu, Kai; Zhang, Ke; Pan, Jun; Ye, Qinda; Atasoylu, Onur; Behshad, Elham; He, Xin; Conlen, Patricia; Stump, Kristine; Ye, Min; Diamond, Sharon; Covington, Maryanne; Yeleswaram, Swamy; Yao, Wenqing 分享 收藏 Discovery of Pyrazolopyridine Derivatives as HPK1 InhibitorsYe, Qinda; Liu, Kai; Ye, Hai-Fen; Pan, Jun; Sokolsky, Alexander; Wang, Anlai; Zhang, Ke; Hummel, Joshua R.; Kong, Ling; Behshad, Elham; He, Xin; Conlen, Patricia; Stump, Kristine; Ye, Min; Diamond, Sharon; Covington, Maryanne; Yeleswaram, Swamy; Atasoylu, Onur; Vechorkin, Oleg; Yao, Wenqing 分享 收藏 Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3Shvartsbart, Artem; Roach, Jeremy J.; Witten, Michael R.; Koblish, Holly; Harris, Jennifer J.; Covington, Maryanne; Hess, Rodrigo; Lin, Luping; Frascella, Michelle; Truong, Lisa; Leffet, Lynn; Conlen, Patricia; Beshad, Elham; Klabe, Ron; Katiyar, Kamna; Kaldon, Laura; Young-Sciame, Ruth; He, Xin; Petusky, Susan; Chen, Kwang-Jong; Horsey, April; Lei, Hsiang-Ting; Epling, Leslie B.; Deller, Marc C.; Vechorkin, Oleg; Yao, Wenqing 分享 收藏 Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 InhibitorsSokolsky, Alexander; Winterton, Sarah; Kennedy, Keith; Drake, Katherine; Stump, Kristine; Huo, Lu; Lo, Yvonne; Ye, Min; Covington, Maryanne; Diamond, Sharon; Yang, Yan-ou; Kim, Sunkyu; Yeleswaram, Swamy; Wu, Liangxing; Yao, Wenqing 分享 收藏 Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2发现新型吡唑并嘧啶作为ALK2的有效，选择性和口服生物利用度抑制剂Nguyen, Minh H.; Atasoylu, Onur; Wu, Liangxing; Kapilashrami, Kanishk; Pusey, Michelle; Gallagher, Karen; Lai, Cheng-Tsung; Zhao, Peng; Barbosa, Joseph; Liu, Kai; He, Chunhong; Zhang, Colin; Styduhar, Evan D.; Witten, Michael R.; Chen, Yaoyu; Lin, Luping; Yang, Yan-ou; Covington, Maryanne; Diamond, Sharon; Yeleswaram, Swamy; Yao, Wenqing 分享 收藏 INCB090244, A POTENT SMALL MOLECULE THAT INHIBITS THE PD-L1/PD-1 AXIS AND FUNCTIONS SIMILARLY TO PD-L1 ANTIBODIESRios-Doria, Jonathan; Volgina, Alla; Gokhale, Prafulla; Liu, Hao; Stevens, Christina; Zolotarjova, Nina; DiMatteo, Darlise; Kapilashrami, Kanishk; Behshad, Elham; Thekkat, Pramod; Yang, Gengjie; Hall, Leslie; Kanellopoulou, Chrysi; Rupar, Mark; Maddage, Christopher; Horsey, April; Burke, Krista; Yang, Yan-ou; Covington, Maryanne; Wang, Steve; Liu, Phillip; Wynn, Richard; Reardon, David; Koblish, Holly 分享 收藏 Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) InhibitorWu, Liangxing; Zhang, Colin; He, Chunhong; Qian, Dingquan; Lu, Liang; Sun, Yaping; Xu, Meizhong; Zhuo, Jincong; Liu, Phillip C. C.; Klabe, Ronald; Wynn, Richard; Covington, Maryanne; Gallagher, Karen; Leffet, Lynn; Bowman, Kevin; Diamond, Sharon; Koblish, Holly; Zhang, Yue; Soloviev, Maxim; Hollis, Gregory; Burn, Timothy C.; Scherle, Peggy; Yeleswaram, Swamy; Huber, Reid; Yao, Wenqing 分享 收藏 Developing a JAK Inhibitor for Targeted Local Delivery: Ruxolitinib CreamSmith, Paul; Yao, Wenqing; Shepard, Stacey; Covington, Maryanne; Lee, Jim; Lofland, Jennifer; Naim, Ahmad; Sheth, Trupti; Parikh, Bhavnish; Yeleswaram, Swamy 分享 收藏 A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted ActivityRios-Doria, Jonathan; Favata, Margaret; Lasky, Kerri; Feldman, Patricia; Lo, Yvonne; Yang, Gengjie; Stevens, Christina; Wen, Xiaoming; Sehra, Sarita; Katiyar, Kamna; Liu, Ke; Wynn, Richard; Harris, Jennifer J.; Ye, Min; Spitz, Susan; Wang, Xiaozhao; He, Chunhong; Li, Yun-Long; Yao, Wenqing; Covington, Maryanne; Scherle, Peggy; Koblish, Holly 分享 收藏 Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseasesCovington, Maryanne; He, Xin; Scuron, Monika; Li, Jun; Collins, Robert; Juvekar, Ashish; Shin, Niu; Favata, Margaret; Gallagher, Karen; Sarah, Sarala; Xue, Chu-biao; Peel, Michael; Burke, Krista; Oliver, Julian; Fay, Brittany; Yao, Wenqing; Huang, Taisheng; Scherle, Peggy; Diamond, Sharon; Newton, Robert; Zhang, Yan; Smith, Paul 分享 收藏 The role of HPK1 in the regulation of T cell function and anti-tumor immune activityChen, Yaoyu; Rios-Doria, Jonathan; Pusey, Michelle; Lasky, Kerri; Ye, Min; Thekkat, Pramod; Gallagher, Karen; Stump, Kristine; Conlen, Patricia; Gardiner, Christine; Wang, Hui; Sokolsky, Alexander; Rupar, Mark; Lin, Luping; Behshad, Elham; Covington, Maryanne; Koblish, Holly; Vechorkin, Oleg; Yao, Wenqing; Kim, Sunkyu; Chen, Yingnan 分享 收藏 Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell MalignancyShin, Niu; Stubbs, Matthew; Koblish, Holly; Yue, Eddy W.; Soloviev, Maxim; Douty, Brent; Wang, Kathy He; Wang, Qian; Gao, Mingming; Feldman, Patricia; Yang, Gengjie; Hall, Leslie; Hansbury, Michael; O'Connor, Sybil; Leffet, Lynn; Collins, Robert; Katiyar, Kamna; He, Xin; Waeltz, Paul; Collier, Paul; Lu, Jin; Li, Yun-Long; Li, Yanlong; Liu, Phillip C. C.; Burn, Timothy; Covington, Maryanne; Diamond, Sharon; Shuey, Dana; Roberts, Alan; Yeleswaram, Swamy; Hollis, Greg; Metcalf, Brian; Yao, Wenqing; Huber, Reid; Combs, Andrew; Newton, Robert; Scherle, Peggy 分享 收藏 INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)INCB050465 (Parsaclisib)，一种新型的下一代磷酸肌醇3-激酶 δ (PI3Kδ) 抑制剂Yue, Eddy W.; Li, Yun-Long; Douty, Brent; He, Chunhong; Mei, Song; Wayland, Brian; Maduskuie, Thomas; Falahatpisheh, Nikoo; Sparks, Richard B.; Polam, Padmaja; Zhu, Wenyu; Glenn, Joseph; Feng, Hao; Zhang, Ke; Li, Yanlong; He, Xin; Katiyar, Kamna; Covington, Maryanne; Feldman, Patricia; Shin, Niu; Wang, Kathy He; Diamond, Sharon; Li, Yu; Koblish, Holly K.; Hall, Leslie; Scherle, Peggy; Yeleswaram, Swamy; Xue, Chu-Biao; Metcalf, Brian; Combs, Andrew P.; Yao, Wenqing 分享 收藏 Preclinical characterization of potent and selective oral PD-L1 small-molecule antagonistsWang, Liang-Chuan S.; Koblish, Holly; Zhang, Yue; Kulkarni, Ashwini; Covington, Maryanne; Gallagher, Karen; Yang, Gengjie; Rios-Doria, Jonathan; Stevens, Christina; Hansbury, Michael; O'Connor, Sybil; Yang, Yan-ou; Diamond, Sharon; Burke, Krista; Xiao, Kaijiong; Li, Jingwei; Yao, Wenqing; Wu, Liangxing; Scherle, Peggy; Hollis, Gregory; Huber, Reid 分享 收藏 
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