Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based... von Gong, Hua, Weinstein, David S., Lu, Zhonghui, Duan, James J.-W., Stachura, Sylwia, Haque, Lauren, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Khan, Javed, Camac, Dan, Sack, John S., Pudzianowski, Andrew, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Borowski, Virna, Xie, Jenny H., Sun, Huadong, D'Arienzo, Celia, Dabros, Marta, Galella, Michael A., Wang, Faye, Weigelt, Carolyn A., Zhao, Qihong, Foster, William, Somerville, John E., Salter-Cid, Luisa M., Barrish, Joel C., Carter, Percy H., Dhar, T.G. Murali

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Loopholes and missing links in protein modeling von Rossi, Karen A., Weigelt, Carolyn A., Nayeem, Akbar, Krystek, Stanley R.

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Tricyclic-Carbocyclic RORγt Inverse AgonistsDiscovery of BMS-986313 von Yang, Michael G, Beaudoin-Bertrand, Myra, Xiao, Zili, Marcoux, David, Weigelt, Carolyn A, Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Li, Sha, Shuster, David J, Xie, Jenny H, Sherry, Tara, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Khandelwal, Purnima, Karmakar, Ananta, Basha, Mushkin, Babu, Venkatesh, Gupta, Arun Kumar, Mathur, Arvind, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T. G. Murali

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Rationally Designed, Conformationally Constrained Inverse Agonists of RORγtIdentification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy von Marcoux, David, Duan, James J.-W, Shi, Qing, Cherney, Robert J, Srivastava, Anurag S, Cornelius, Lyndon, Batt, Douglas G, Liu, Qingjie, Beaudoin-Bertrand, Myra, Weigelt, Carolyn A, Khandelwal, Purnima, Vishwakrishnan, Sureshbabu, Selvakumar, Kumaravel, Karmakar, Ananta, Gupta, Arun Kumar, Basha, Mushkin, Ramlingam, Sridharan, Manjunath, Naveen, Vanteru, Sridhar, Karmakar, Sukhen, Maddala, Nageswara, Vetrichelvan, Muthalagu, Gupta, Anuradha, Rampulla, Richard A, Mathur, Arvind, Yip, Shiuhang, Li, Peng, Wu, Dauh-Rurng, Khan, Javed, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Li, Sha, Shuster, David J, Borowski, Virna, Xie, Jenny H, McIntyre, Kim W, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Hynes, John, Tino, Joseph A, Macor, John E, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Carter, Percy H, Dhar, T. G. Murali

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Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists von Marcoux, David, Bertrand, Myra Beaudoin, Weigelt, Carolyn A., Yip, Shiuhang, Galella, Michael, Park, Hyunsoo, Wu, Dauh-Rurng, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Li, Sha, Hynes, John, Tino, Joseph A., Zhao, Qihong, Dhar, T.G. Murali

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Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists von Duan, James J.-W, Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Weigelt, Carolyn A, Sack, John S, Khan, Javed, Ruzanov, Max, Galella, Michael A, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Shuster, David J, Borowski, Virna, Xie, Jenny H, Zhang, Lisa, Vanteru, Sridhar, Gupta, Arun Kumar, Mathur, Arvind, Zhao, Qihong, Foster, William, Salter-Cid, Luisa M, Carter, Percy H, Dhar, T. G. Murali

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Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists von Harikrishnan, Lalgudi S., Gill, Patrice, Kamau, Muthoni G., Qin, Lan-Ying, Ruan, Zheming, O'Malley, Daniel, Huynh, Tram, Stachura, Sylwia, Cavallaro, Cullen L., Lu, Zhonghui, J.-W. Duan, James, Weigelt, Carolyn A., Sack, John S., Ruzanov, Max, Khan, Javed, Gururajan, Murali, Wong, Jessica J., Huang, Yanling, Yarde, Melissa, Li, Zhuyin, Chen, Cliff, Sun, Huadong, Borowski, Virna, Murtaza, Anwar, Fink, Brian E.

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Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists von Jiang, Bin, Duan, James J.-W., Stachura, Sylwia, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Weigelt, Carolyn A., Khan, Javed, Sack, John S., Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Galella, Michael A., Mathur, Arvind, Zhao, Qihong, Salter-Cid, Luisa M., Carter, Percy H., Dhar, T.G. Murali

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Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists von Ruan, Zheming, Park, Peter K., Wei, Donna, Purandare, Ashok, Wan, Honghe, O'Malley, Daniel, Stachura, Sylwia, Perez, Heidi, Cavallaro, Cullen L., Weigelt, Carolyn A., Sack, John S., Ruzanov, Max, Khan, Javed, Gururajan, Murali, Wong, Jessica J., Huang, Yanling, Yarde, Melissa, Li, Zhuyin, Chen, Cliff, Sun, Huadong, Borowski, Virna, Xie, Jenny H., Anthony, Monique, Agler, Michele, Fink, Brian E., Harikrishnan, Lalgudi S.

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Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists von Lu, Zhonghui, Duan, James J.-W., Xiao, Haiyun, Neels, James, Wu, Dauh-Rurng, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, An, Yongmi, Yarde, Melissa, Karmakar, Ananta, Vishwakrishnan, Sureshbabu, Baratam, Venkata, Shankarappa, Harisha, Vanteru, Sridhar, Babu, Venkatesh, Basha, Mushkin, Kumar Gupta, Arun, Kumaravel, Selvakumar, Mathur, Arvind, Zhao, Qihong, Salter-Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.

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Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist von Cherney, Robert J., Cornelius, Lyndon A. M., Srivastava, Anurag, Weigelt, Carolyn A., Marcoux, David, Duan, James J.-W., Shi, Qing, Batt, Douglas G., Liu, Qingjie, Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John, Khan, Javed, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Mathur, Arvind, Li, Sha, Shuster, David, Khandelwal, Purnima, Borowski, Virna, Xie, Jenny, Obermeier, Mary, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Tino, Joseph A., Macor, John E., Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Carter, Percy H., Dhar, T. G. Murali

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Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists – Exploring C6 and C8 SAR using late-stage functionalization von Shi, Qing, Xiao, Zili, Yang, Michael G., Marcoux, David, Cherney, Robert J., Yip, Shiuhang, Li, Peng, Wu, Dauh-Rurng, Weigelt, Carolyn A., Sack, John, Khan, Javed, Ruzanov, Max, Wang, Jinhong, Yarde, Melissa, Ellen Cvijic, Mary, Li, Sha, Shuster, David J., Xie, Jenny, Sherry, Tara, Obermeier, Mary, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Chacko, Silvi, Shu, Yue-Zhong, Khandelwal, Purnima, Hynes, John, Tino, Joseph A., Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T.G. Murali

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Discovery of 2,6–difluorobenzyl ether series of phenyl ((R)–3–phenylpyrrolidin–3–yl)sulfones as surprisingly potent, selective and orally bioavailable RORγt inverse agonists... von Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Stachura, Sylwia, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, Wu, Dauh–Rurng, Yarde, Melissa, Shen, Ding–Ren, Zhao, Qihong, Salter–Cid, Luisa M., Carter, Percy H., Murali Dhar, T.G.

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Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach von Liu, Qingjie, Batt, Douglas G, Weigelt, Carolyn A, Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Li, Sha, Shuster, David J, Xie, Jenny H, Sherry, Tara, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Khandelwal, Purnima, Tino, Joseph A, Macor, John E, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T. G. Murali

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Closing the side-chain gap in protein loop modeling von Rossi, Karen A., Nayeem, Akbar, Weigelt, Carolyn A., Krystek, Stanley R.

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Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors von Qin, Lan-Ying, Ruan, Zheming, Cherney, Robert J., Dhar, T.G. Murali, Neels, James, Weigelt, Carolyn A., Sack, John S., Srivastava, Anurag S., Cornelius, Lyndon A.M., Tino, Joseph A., Stefanski, Kevin, Gu, Xiaomei, Xie, Jenny, Susulic, Vojkan, Yang, Xiaoxia, Yarde-Chinn, Melissa, Skala, Stacey, Bosnius, Ruth, Goldstein, Christine, Davies, Paul, Ruepp, Stefan, Salter-Cid, Luisa, Bhide, Rajeev S., Poss, Michael A.

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Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis von Liu, Qingjie, Xiao, Hai-Yun, Batt, Douglas G, Xiao, Zili, Zhu, Yeheng, Yang, Michael G, Li, Ning, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S, Weigelt, Carolyn A, Wang, Jinhong, Li, Sha, Shuster, David J, Xie, Jenny H, Song, Yunling, Sherry, Tara, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Chacko, Silvi, Khandelwal, Purnima, Dudhgaonkar, Shailesh, Rudra, Anjuman, Nagar, Jignesh, Murali, Venkata, Govindarajan, Arun, Denton, Rex, Zhao, Qihong, Meanwell, Nicholas A, Borzilleri, Robert, Dhar, T. G. Murali

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Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors von Glunz, Peter W., Cheng, Xuhong, Cheney, Daniel L., Weigelt, Carolyn A., Wei, Anzhi, Luettgen, Joseph M., Wong, Pancras C., Wexler, Ruth R., Priestley, E. Scott

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Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors von Meng, Wei, Brigance, Robert P, Chao, Hannguang J, Fura, Aberra, Harrity, Thomas, Marcinkeviciene, Jovita, O’Connor, Stephen P, Tamura, James K, Xie, Dianlin, Zhang, Yaqun, Klei, Herbert E, Kish, Kevin, Weigelt, Carolyn A, Turdi, Huji, Wang, Aiying, Zahler, Robert, Kirby, Mark S, Hamann, Lawrence G

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Nonbenzamidine acylsulfonamide tissue factor–factor VIIa inhibitors von Glunz, Peter W., Zhang, Xiaojun, Zou, Yan, Delucca, Indawati, Nirschl, Alexandra H., Cheng, Xuhong, Weigelt, Carolyn A., Cheney, Daniel L., Wei, Anzhi, Anumula, Rushith, Luettgen, Joseph M., Rendina, Alan R., Harpel, Mark, Luo, Gang, Knabb, Robert, Wong, Pancras C., Wexler, Ruth R., Priestley, E. Scott

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