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Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK) Watterson, Scott H.; Liu, Qingjie; Bertrand, Myra Beaudoin; Batt, Douglas G.; Li, Ling; Pattoli, Mark A.; Skala, Stacey; Cheng, Lihong; Obermeier, Mary T.; Moore, Robin; Yang, Zheng; Vickery, Rodney; Elzinga, Paul A.; Discenza, Lorell; D'Arienzo, Celia; Gillooly, Kathleen M.; Taylor, Tracy L.; Pulicicchio, Claudine; Zhang, Yifan; Heimrich, Elizabeth; McIntyre, Kim W.; Ruan, Qian; Westhouse, Richard A.; Catlett, Ian M.; Zheng, Naiyu; Chaudhry, Charu; Dai, Jun; Galella, Michael A.; Tebben, Andrew J.; Pokross, Matt; Li, Jianqing; Zhao, Rulin; Smith, Daniel; Rampulla, Richard; Allentoff, Alban; Wallace, Michael A.; Mathur, Arvind; Salter-Cid, Luisa; Macor, John E.; Carter, Percy H.; Fura, Aberra; Burke, James R.; Tino, Joseph A. Share Save
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Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers Watterson, Scott H.; De Lucca, George V.; Shi, Qing; Langevine, Charles M.; Liu, Qingjie; Batt, Douglas G.; Bertrand, Myra Beaudoin; Gong, Hua; Dai, Jun; Yip, Shiuhang; Li, Peng; Sun, Dawn; Wu, Dauh-Rurng; Wang, Chunlei; Zhang, Yingru; Traeger, Sarah C.; Pattoli, Mark A.; Skala, Stacey; Cheng, Lihong; Obermeier, Mary T.; Vickery, Rodney; Discenza, Lorell N.; D'Arienzo, Celia J.; Zhang, Yifan; Heimrich, Elizabeth; Gillooly, Kathleen M.; Taylor, Tracy L.; Pulicicchio, Claudine; McIntyre, Kim W.; Galena, Michael A.; Tebben, Andy J.; Muckelbauer, Jodi K.; Chang, ChiehYing; Rampulla, Richard; Mathur, Arvind; Salter-Cid, Luisa; Barrish, Joel C.; Carter, Percy H.; Fura, Aberra; Burke, James R.; Tino, Joseph A. Share Save
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177) De Lucca, George V.; Shi, Qing; Liu, Qingjie; Batt, Douglas G.; Bertrand, Myra Beaudoin; Rampulla, Rick; Mathur, Arvind; Discenza, Lorell; D'Arienzo, Celia; Dai, Jun; Obermeier, Mary; Vickery, Rodney; Zhang, Yingru; Yang, Zheng; Marathe, Punit; Tebben, Andrew J.; Muckelbauer, Jodi K.; Chang, ChiehYing J.; Zhang, Huiping; Gillooly, Kathleen; Taylor, Tracy; Pattoli, Mark A.; Skala, Stacey; Kukral, Daniel W.; McIntyre, Kim W.; Salter-Cid, Luisa; Fura, Aberra; Burke, James R.; Banish, Joel C.; Carter, Percy H.; Tino, Joseph A. Share Save
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series Watterson, Scott H.; Guo, Junqing; Spergel, SteiTe H.; Langevine, Charles M.; Moquin, Robert V.; Shen, Ding Ren; Yarde, Melissa; Cvijic, Mary Ellen; Banas, Dana; Liu, Richard; Suchard, Suzanne J.; Gillooly, Kathleen; Taylor, Tracy; Rex-Rabe, Sandra; Shuster, David J.; McIntyre, Kim W.; Cornelius, Georgia; D'Arienzo, Celia; Marino, Anthony; Balimane, Praveen; Warrack, Bethanne; Salter-Cid, Luisa; McKinnon, Murray; Barrish, Joel C.; Carter, Percy H.; Pitts, William J.; Xie, Jenny; Dyckman, Alaric J. Share Save