Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor
Gray, David L, Allen, John A, Mente, Scot, O'Connor, Rebecca E, DeMarco, George J, Efremov, Ivan, Tierney, Patrick, Volfson, Dmitri, Davoren, Jennifer, Guilmette, Edward, Salafia, Michelle, Kozak, Rouba, Ehlers, Michael D
Published in Nature communications (14.02.2018)
Published in Nature communications (14.02.2018)
Get full text
Journal Article
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation
McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
Get full text
Journal Article
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase
Butler, Christopher R., Beck, Elizabeth M., Harris, Anthony, Huang, Zhen, McAllister, Laura A., am Ende, Christopher W., Fennell, Kimberly, Foley, Timothy L., Fonseca, Kari, Hawrylik, Steven J., Johnson, Douglas S., Knafels, John D., Mente, Scot, Noell, G. Stephen, Pandit, Jayvardhan, Phillips, Tracy B., Piro, Justin R., Rogers, Bruce N., Samad, Tarek A., Wang, Jane, Wan, Shuangyi, Brodney, Michael A.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
Get full text
Journal Article
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor
Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
Get full text
Journal Article
Discovery, SAR, and Pharmacokinetics of a Novel 3-Hydroxyquinolin-2(1H)-one Series of Potent d-Amino Acid Oxidase (DAAO) Inhibitors
Duplantier, Allen J, Becker, Stacey L, Bohanon, Michael J, Borzilleri, Kris A, Chrunyk, Boris A, Downs, James T, Hu, Lain-Yen, El-Kattan, Ayman, James, Larry C, Liu, Shenping, Lu, Jiemin, Maklad, Noha, Mansour, Mahmoud N, Mente, Scot, Piotrowski, Mary A, Sakya, Subas M, Sheehan, Susan, Steyn, Stefanus J, Strick, Christine A, Williams, Victoria A, Zhang, Lei
Published in Journal of medicinal chemistry (11.06.2009)
Published in Journal of medicinal chemistry (11.06.2009)
Get full text
Journal Article
Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State
Kurnik, Martin, Sahin, Cagla, Andersen, Camilla Bertel, Lorenzen, Nikolai, Giehm, Lise, Mohammad-Beigi, Hossein, Jessen, Christian Moestrup, Pedersen, Jan Skov, Christiansen, Gunna, Petersen, Steen Vang, Staal, Roland, Krishnamurthy, Girija, Pitts, Keith, Reinhart, Peter H, Mulder, Frans A A, Mente, Scot, Hirst, Warren D, Otzen, Daniel E
Published in Cell chemical biology (15.11.2018)
Published in Cell chemical biology (15.11.2018)
Get full text
Journal Article
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M 4 Muscarinic Acetylcholine Receptor
Butler, Christopher R., Popiolek, Michael, McAllister, Laura A., LaChapelle, Erik A., Kramer, Melissa, Beck, Elizabeth M., Mente, Scot, Brodney, Michael A., Brown, Matthew, Gilbert, Adam, Helal, Chris, Ogilvie, Kevin, Starr, Jeremy, Uccello, Daniel, Grimwood, Sarah, Edgerton, Jeremy, Garst-Orozco, Jonathan, Kozak, Rouba, Lotarski, Susan, Rossi, Amie, Smith, Deborah, O’Connor, Rebecca, Lazzaro, John, Steppan, Claire, Steyn, Stefanus J.
Published in Journal of medicinal chemistry (11.07.2024)
Published in Journal of medicinal chemistry (11.07.2024)
Get full text
Journal Article
Dopamine D1 receptor-agonist interactions: A mutagenesis and homology modeling study
Mente, Scot, Guilmette, Edward, Salafia, Michelle, Gray, David
Published in Bioorganic & medicinal chemistry letters (15.05.2015)
Published in Bioorganic & medicinal chemistry letters (15.05.2015)
Get full text
Journal Article
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor
Butler, Christopher R., Popiolek, Michael, McAllister, Laura A., LaChapelle, Erik A., Kramer, Melissa, Beck, Elizabeth M., Mente, Scot, Brodney, Michael A., Brown, Matthew, Gilbert, Adam, Helal, Chris, Ogilvie, Kevin, Starr, Jeremy, Uccello, Daniel, Grimwood, Sarah, Edgerton, Jeremy, Garst-Orozco, Jonathan, Kozak, Rouba, Lotarski, Susan, Rossi, Amie, Smith, Deborah, O’Connor, Rebecca, Lazzaro, John, Steppan, Claire, Steyn, Stefanus J.
Published in Journal of medicinal chemistry (11.07.2024)
Published in Journal of medicinal chemistry (11.07.2024)
Get full text
Journal Article
Mapping the Binding Site of BMS-708163 on γ-Secretase with Cleavable Photoprobes
Gertsik, Natalya, am Ende, Christopher W., Geoghegan, Kieran F., Nguyen, Chuong, Mukherjee, Paramita, Mente, Scot, Seneviratne, Uthpala, Johnson, Douglas S., Li, Yue-Ming
Published in Cell chemical biology (19.01.2017)
Published in Cell chemical biology (19.01.2017)
Get full text
Journal Article
NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
Drilon, Alexander, Horan, Joshua C, Tangpeerachaikul, Anupong, Besse, Benjamin, Ou, Sai-Hong Ignatius, Gadgeel, Shirish M, Camidge, D Ross, van der Wekken, Anthonie J, Nguyen-Phuong, Linh, Acker, Adam, Keddy, Clare, Nicholson, Katelyn S, Yoda, Satoshi, Mente, Scot, Sun, Yuting, Soglia, John R, Kohl, Nancy E, Porter, James R, Shair, Matthew D, Zhu, Viola, Davare, Monika A, Hata, Aaron N, Pelish, Henry E, Lin, Jessica J
Published in Cancer discovery (01.03.2023)
Published in Cancer discovery (01.03.2023)
Get full text
Journal Article
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
Lin, Jessica J., Horan, Joshua C., Tangpeerachaikul, Anupong, Swalduz, Aurélie, Valdivia, Augusto, Johnson, Melissa L., Besse, Benjamin, Camidge, D. Ross, Fujino, Toshio, Yoda, Satoshi, Nguyen-Phuong, Linh, Mizuta, Hayato, Bigot, Ludovic, Nobre, Catline, Lee, Jii Bum, Yu, Mi Ra, Mente, Scot, Sun, Yuting, Kohl, Nancy E., Porter, James R., Shair, Matthew D., Zhu, Viola W., Felip, Enriqueta, Cho, Byoung Chul, Friboulet, Luc, Hata, Aaron N., Pelish, Henry E., Drilon, Alexander
Published in Cancer discovery (13.09.2024)
Published in Cancer discovery (13.09.2024)
Get full text
Journal Article
헤테로방향족 거대환식 에터 화학치료제
TANGPEERACHAIKUL ANUPONG, MENTE SCOT RICHARD, TANG XINXING, PELISH HENRY EFREM, SHAIR MATTHEW D, HORAN JOSHUA COURTNEY
Year of Publication 09.02.2023
Get full text
Year of Publication 09.02.2023
Patent
헤테로방향족 거대환식 에터 화학치료제
TANGPEERACHAIKUL ANUPONG, MENTE SCOT RICHARD, TANG XINXING, PELISH HENRY EFREM, SHAIR MATTHEW D, HORAN JOSHUA COURTNEY
Year of Publication 10.01.2023
Get full text
Year of Publication 10.01.2023
Patent
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist
Schnute, Mark E, Wennerstål, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R, Bolten, Charles W, Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P, Crouse, Kimberly, Färnegårdh, Mathias, Fennell, Kimberly F, Fish, Susan, Flick, Andrew C, Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K, Heasley, Steven E, Hegen, Martin, Hromockyj, Alexander E, Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Björn, Kiefer, James R, Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G, Kyne, Jr, Robert E, Li, Wei, Löfstedt, Joakim, Long, Scott A, Menard, Carol A, Mente, Scot, Messing, Dean, Meyers, Marvin J, Napierata, Lee, Nöteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J, Prinsen, Michael J, Rhönnstad, Patrik, Backström-Rydin, Eva, Sandberg, Johnny, Sandström, Maria, Shah, Falgun, Sjöberg, Maria, Sundell, Aron, Taylor, Alexandria P, Thorarensen, Atli, Trujillo, John I, Trzupek, John D, Unwalla, Ray, Vajdos, Felix F, Weinberg, Robin A, Wood, David C, Xing, Li, Zamaratski, Edouard, Zapf, Christoph W, Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
Get full text
Journal Article
Discovery of 3-Cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yObenzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor Related Orphan Receptor C2 Inverse Agonist
Schnute, Mark E., Wennerstal, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R., Bolten, Charles W., Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P., Crouse, Kimberly, Farnegardh, Mathias, Fennell, Kimberly F., Fish, Susan, Flick, Andrew C., Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K., Heasley, Steven E., Hegen, Martin, Hromockyj, Alexander E., Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Bjorn, Kiefer, James R., Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G., Kyne, Robert E., Li, Wei, Lofstedt, Joakim, Long, Scott A., Menard, Carol A., Mente, Scot, Messing, Dean, Meyers, Marvin J., Napierata, Lee, Noteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J., Prinsen, Michael J., Rhonnstad, Patrik, Backstrom-Rydin, Eva, Sandberg, Johnny, Sandstrom, Maria, Shah, Falgun, Sjoberg, Maria, Sundell, Aron, Taylor, Alexandria P., Thorarensen, Atli, Trujillo, John I., Trzupek, John D., Unwalla, Ray, Vajdos, Felix F., Weinberg, Robin A., Wood, David C., Xing, Li, Zamaratski, Edouard, Zapf, Christoph W., Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
Get full text
Journal Article
Discovery of Two Clinical Histamine H-3 Receptor Antagonists: trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)-phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764)
Wager, Travis T., Pettersen, Betty A., Schmidt, Anne W., Spracklin, Douglas K., Mente, Scot, Butler, Todd W., Howard, Harry, Lettiere, Daniel J., Rubitski, David M., Wong, Diane F., Nedza, Frank M., Nelson, Frederick R., Rollema, Hans, Raggon, Jeffrey W., Aubrecht, Jiri, Freeman, Jody K., Marcek, John M., Cianfrogna, Julie, Cook, Karen W., James, Larry C., Chatman, Linda A., Iredale, Philip A., Banker, Michael J., Homiski, Michael L., Munzner, Jennifer B., Chandrasekaran, Rama Y.
Published in Journal of medicinal chemistry (10.11.2011)
Published in Journal of medicinal chemistry (10.11.2011)
Get full text
Journal Article
EGFR 돌연변이를 지니는 암을 치료하기 위한 아미노-치환된 헤테로사이클
GERARD BAUDOUIN, ANDREWS KRISTIN LYNNE, TANGPEERACHAIKUL ANUPONG, SUN YUTING, MENTE SCOT RICHARD, PELISH HENRY EFREM, SHAIR MATTHEW D, HORAN JOSHUA COURTNEY
Year of Publication 18.12.2023
Get full text
Year of Publication 18.12.2023
Patent