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The novel ghrelin receptor inverse agonist PF-5190457 administered with alcohol: preclinical safety experiments and a phase 1b human laboratory study
Lee, Mary R., Tapocik, Jenica D., Ghareeb, Mwlod, Schwandt, Melanie L., Dias, Alexandra A., Le, April N., Cobbina, Enoch, Farinelli, Lisa A., Bouhlal, Sofia, Farokhnia, Mehdi, Heilig, Markus, Akhlaghi, Fatemeh, Leggio, Lorenzo
Published in Molecular psychiatry (01.02.2020)
Published in Molecular psychiatry (01.02.2020)
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Journal Article
Pharmacokinetics and pharmacodynamics of PF‐05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects
Denney, William S., Sonnenberg, Gabriele E., Carvajal‐Gonzalez, Santos, Tuthill, Theresa, Jackson, V. Margaret
Published in British journal of clinical pharmacology (01.02.2017)
Published in British journal of clinical pharmacology (01.02.2017)
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Journal Article
Assessment of structure-activity relationships and biased agonism at the Mu opioid receptor of novel synthetic opioids using a novel, stable bio-assay platform
Vasudevan, Lakshmi, Vandeputte, Marthe, Deventer, Marie, Wouters, Elise, Cannaert, Annelies, Stove, Christophe P.
Published in Biochemical pharmacology (01.07.2020)
Published in Biochemical pharmacology (01.07.2020)
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Journal Article
Towards a new combination therapy for tuberculosis with next generation benzothiazinones
Makarov, Vadim, Lechartier, Benoit, Zhang, Ming, Neres, João, van der Sar, Astrid M, Raadsen, Susanne A, Hartkoorn, Ruben C, Ryabova, Olga B, Vocat, Anthony, Decosterd, Laurent A, Widmer, Nicolas, Buclin, Thierry, Bitter, Wilbert, Andries, Koen, Pojer, Florence, Dyson, Paul J, Cole, Stewart T
Published in EMBO molecular medicine (01.03.2014)
Published in EMBO molecular medicine (01.03.2014)
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Journal Article
Occupancy of Nociceptin/Orphanin FQ Peptide Receptors by the Antagonist LY2940094 in Rats and Healthy Human Subjects
Raddad, Eyas, Chappell, Amy, Meyer, Jeffery, Wilson, Alan, Ruegg, Charles E, Tauscher, Johannes, Statnick, Michael A, Barth, Vanessa, Zhang, Xin, Verfaille, Steven J
Published in Drug metabolism and disposition (01.09.2016)
Published in Drug metabolism and disposition (01.09.2016)
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Journal Article
KAE609 (Cipargamin), a New Spiroindolone Agent for the Treatment of Malaria: Evaluation of the Absorption, Distribution, Metabolism, and Excretion of a Single Oral 300-mg Dose of [14C]KAE609 in Healthy Male Subjects
Huskey, Su-Er W., Zhu, Chun-qi, Fredenhagen, Andreas, Kühnöl, Jürgen, Luneau, Alexandre, Jian, Zhigang, Yang, Ziping, Miao, Zhuang, Yang, Fan, Jain, Jay P., Sunkara, Gangadhar, Mangold, James B., Stein, Daniel S.
Published in Drug metabolism and disposition (01.05.2016)
Published in Drug metabolism and disposition (01.05.2016)
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The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470)
Hamdouchi, Chafiq, Kahl, Steven D, Patel Lewis, Anjana, Cardona, Guemalli R, Zink, Richard W, Chen, Keyue, Eessalu, Thomas E, Ficorilli, James V, Marcelo, Marialuisa C, Otto, Keith A, Wilbur, Kelly L, Lineswala, Jayana P, Piper, Jared L, Coffey, D. Scott, Sweetana, Stephanie A, Haas, Joseph V, Brooks, Dawn A, Pratt, Edward J, Belin, Ruth M, Deeg, Mark A, Ma, Xiaosu, Cannady, Ellen A, Johnson, Jason T, Yumibe, Nathan P, Chen, Qi, Maiti, Pranab, Montrose-Rafizadeh, Chahrzad, Chen, Yanyun, Reifel Miller, Anne
Published in Journal of medicinal chemistry (22.12.2016)
Published in Journal of medicinal chemistry (22.12.2016)
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Journal Article
Identification of a Human Whole Blood–Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo
Xu, Xiaoping, Goyal, Navin, Costell, Melissa H., Roethke, Theresa, James, Christian H., Thorneloe, Kevin S., Patterson, Jaclyn, Stoy, Patrick, Goodman, Krista, Sprecher, Dennis L., Behm, David J.
Published in The Journal of pharmacology and experimental therapeutics (01.03.2021)
Published in The Journal of pharmacology and experimental therapeutics (01.03.2021)
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Journal Article
Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects
Wang, Jing, Zhang, Zhi-Yi, Lu, Sharon, Powers, Dan, Kansra, Vikram, Wang, Xiaodong
Published in Supportive care in cancer (01.03.2019)
Published in Supportive care in cancer (01.03.2019)
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Journal Article
Optimization of Antitumor Modulators of Pre-mRNA Splicing
Lagisetti, Chandraiah, Palacios, Gustavo, Goronga, Tinopiwa, Freeman, Burgess, Caufield, William, Webb, Thomas R
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Journal Article
Open-Label, Single-Dose, Parallel-Group Study in Healthy Volunteers To Determine the Drug-Drug Interaction Potential between KAE609 (Cipargamin) and Piperaquine
Stein, Daniel S., Jain, Jay Prakash, Kangas, Michael, Lefèvre, Gilbert, Machineni, Surendra, Griffin, Paul, Lickliter, Jason
Published in Antimicrobial agents and chemotherapy (01.06.2015)
Published in Antimicrobial agents and chemotherapy (01.06.2015)
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Journal Article
Identification and mechanism of action analysis of the new PARP-1 inhibitor 2″-hydroxygenkwanol A
Dal Piaz, Fabrizio, Ferro, Piera, Vassallo, Antonio, Vasaturo, Michele, Forte, Giovanni, Chini, Maria Giovanna, Bifulco, Giuseppe, Tosco, Alessandra, De Tommasi, Nunziatina
Published in Biochimica et biophysica acta (01.09.2015)
Published in Biochimica et biophysica acta (01.09.2015)
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Journal Article
Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor
Lavieri, Robert R, Scott, Sarah A, Selvy, Paige E, Kim, Kwangho, Jadhav, Satyawan, Morrison, Ryan D, Daniels, J. Scott, Brown, H. Alex, Lindsley, Craig W
Published in Journal of medicinal chemistry (23.09.2010)
Published in Journal of medicinal chemistry (23.09.2010)
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Journal Article
Development of the Large-Scale Synthesis of Tetrahydropyran Glycine, a Precursor to the HCV NS5A Inhibitor BMS-986097
Mathur, Arvind, Wang, Bei, Smith, Daniel, Li, Jianqing, Pawluczyk, Joseph, Sun, Jung-Hui, Wong, Michael Kwok, Krishnananthan, Subramaniam, Wu, Dauh-Rurng, Sun, Dawn, Li, Peng, Yip, Shiuhang, Chen, Bang-Chi, Baran, Phil S, Chen, Qi, Lopez, Omar D, Yong, Zhong, Bender, John A, Nguyen, Van N, Romine, Jeffrey L, Laurent, Denis R. St, Wang, Gan, Kadow, John F, Meanwell, Nicholas A, Belema, Makonen, Zhao, Rulin
Published in Journal of organic chemistry (06.10.2017)
Published in Journal of organic chemistry (06.10.2017)
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Journal Article
Hepatotoxicity Observed in Clinical Trials of Aplaviroc (GW873140)
Nichols, W. G., Steel, H. M., Bonny, T., Adkison, K., Curtis, L., Millard, J., Kabeya, K., Clumeck, N.
Published in Antimicrobial Agents and Chemotherapy (01.03.2008)
Published in Antimicrobial Agents and Chemotherapy (01.03.2008)
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Journal Article
(11)C-MK-8278 PET as a tool for pharmacodynamic brain occupancy of histamine 3 receptor inverse agonists
Van Laere, Koenraad J, Sanabria-Bohórquez, Sandra M, Mozley, David P, Burns, Donald H, Hamill, Terence G, Van Hecken, Anne, De Lepeleire, Inge, Koole, Michel, Bormans, Guy, de Hoon, Jan, Depré, Marleen, Cerchio, Kristine, Plalcza, John, Han, Lingling, Renger, John, Hargreaves, Richard J, Iannone, Robert
Published in The Journal of nuclear medicine (1978) (01.01.2014)
Published in The Journal of nuclear medicine (1978) (01.01.2014)
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Journal Article
Spirocyclic Delta Opioid Receptor Agonists for the Treatment of Pain: Discovery of N,N-Diethyl-3-hydroxy-4-(spiro[chromene-2,4′-piperidine]-4-yl) Benzamide (ADL5747)
Le Bourdonnec, Bertrand, Windh, Rolf T., Leister, Lara K., Zhou, Q. Jean, Ajello, Christopher W., Gu, Minghua, Chu, Guo-Hua, Tuthill, Paul A., Barker, William M., Koblish, Michael, Wiant, Daniel D., Graczyk, Thomas M., Belanger, Serge, Cassel, Joel A., Feschenko, Marina S., Brogdon, Bernice L., Smith, Steven A., Derelanko, Michael J., Kutz, Steve, Little, Patrick J., DeHaven, Robert N., DeHaven-Hudkins, Diane L., Dolle, Roland E.
Published in Journal of medicinal chemistry (24.09.2009)
Published in Journal of medicinal chemistry (24.09.2009)
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