Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor
Barrett, Terrance D, Palomino, Heather L, Brondstetter, Theresa I, Kanelakis, Kimon C, Wu, Xiaodong, Haug, Peter V, Yan, Wen, Young, Andrew, Hua, Hong, Hart, Juliet C, Tran, Da-Thao, Venkatesan, Hariharan, Rosen, Mark D, Peltier, Hillary M, Sepassi, Kia, Rizzolio, Michele C, Bembenek, Scott D, Mirzadegan, Tara, Rabinowitz, Michael H, Shankley, Nigel P
Published in Molecular pharmacology (01.06.2011)
Published in Molecular pharmacology (01.06.2011)
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Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4- d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist
Maher, Michael P., Bhattacharya, Anindya, Ao, Hong, Swanson, Nadia, Wu, Nyan-Tsz, Freedman, Jamie, Kansagara, Mena, Scott, Brian, Li, Dong H., Eckert, William A., Liu, Yi, Sepassi, Kia, Rizzolio, Michele, Fitzgerald, Anne, Liu, Jing, Branstetter, Bryan J., Rech, Jason C., Lebsack, Alec D., Breitenbucher, J. Guy, Wickenden, Alan D., Chaplan, Sandra R.
Published in European journal of pharmacology (01.08.2011)
Published in European journal of pharmacology (01.08.2011)
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A Stratified Analysis of Supersaturation and Precipitation Effects Based on the Refined Developability Classification System (rDCS)
Beran, Kristian, Hermans, Eline, Holm, René, Sepassi, Kia, Dressman, Jennifer
Published in Journal of pharmaceutical sciences (01.09.2024)
Published in Journal of pharmaceutical sciences (01.09.2024)
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Journal Article
Effect of Data Quality and Data Quantity on the Estimation of Intrinsic Solubility: Analysis Based on a Single-Source Data Set
Zhao, Jiaxi, Hermans, Eline, Sepassi, Kia, Tistaert, Christophe, Bergström, Christel A. S., Ahmad, Mazen, Larsson, Per
Published in Molecular pharmaceutics (07.10.2024)
Published in Molecular pharmaceutics (07.10.2024)
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A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]triazolo[4,5‑c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate
Chrovian, Christa C, Soyode-Johnson, Akinola, Peterson, Alexander A, Gelin, Christine F, Deng, Xiaohu, Dvorak, Curt A, Carruthers, Nicholas I, Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J, Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J, Bhattacharya, Anindya, Letavic, Michael A
Published in Journal of medicinal chemistry (11.01.2018)
Published in Journal of medicinal chemistry (11.01.2018)
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Design, Synthesis, and Preclinical Evaluation of 3‑Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5‑b]pyridin-2-ones as Selective GluN2B Negative Allosteric Modulators for the Treatment of Mood Disorders
Chrovian, Christa C, Soyode-Johnson, Akinola, Stenne, Brice, Pippel, Daniel J, Schoellerman, Jeffrey, Lord, Brian, Needham, Alexandra S, Xia, Chungfang, Coe, Kevin J, Sepassi, Kia, Schoetens, Freddy, Scott, Brian, Nguyen, Leslie, Jiang, Xiaohui, Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Identification of (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridin-5(4H)‑yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor
Swanson, Devin M, Savall, Brad M, Coe, Kevin J, Schoetens, Freddy, Koudriakova, Tatiana, Skaptason, Judith, Wall, Jessica, Rech, Jason, Deng, Xiahou, De Angelis, Meri, Everson, Anita, Lord, Brian, Wang, Qi, Ao, Hong, Scott, Brian, Sepassi, Kia, Lovenberg, Timothy W, Carruthers, Nicholas I, Bhattacharya, Anindya, Letavic, Michael A
Published in Journal of medicinal chemistry (22.09.2016)
Published in Journal of medicinal chemistry (22.09.2016)
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Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Tichenor, Mark S., Wiener, John J. M., Rao, Navin L., Bacani, Genesis M., Wei, Jianmei, Pooley Deckhut, Charlotte, Barbay, J. Kent, Kreutter, Kevin D., Chang, Leon, Clancy, Kathleen W., Murrey, Heather E., Wang, Weixue, Ahn, Kay, Huber, Michael, Rex, Elizabeth, Coe, Kevin J., Wu, Jiejun, Rui, Haopeng, Sepassi, Kia, Gaudiano, Marcello, Bekkers, Mariette, Cornelissen, Ivo, Packman, Kathryn, Seierstad, Mark, Xiouras, Christos, Bembenek, Scott D., Alexander, Richard, Milligan, Cynthia, Balasubramanian, Sriram, Lebsack, Alec D., Venable, Jennifer D., Philippar, Ulrike, Edwards, James P., Hirst, Gavin
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Journal Article
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1 H -[1,2,3]triazolo[4,5- c ]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate
Chrovian, Christa C., Soyode-Johnson, Akinola, Peterson, Alexander A., Gelin, Christine F., Deng, Xiaohu, Dvorak, Curt A., Carruthers, Nicholas I., Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J., Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J., Bhattacharya, Anindya, Letavic, Michael A.
Published in Journal of medicinal chemistry (11.01.2018)
Published in Journal of medicinal chemistry (11.01.2018)
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Journal Article
Identification of ( R )-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1 H -imidazo[4,5- c ]pyridin-5(4 H )-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor
Swanson, Devin M., Savall, Brad M., Coe, Kevin J., Schoetens, Freddy, Koudriakova, Tatiana, Skaptason, Judith, Wall, Jessica, Rech, Jason, Deng, Xiahou, De Angelis, Meri, Everson, Anita, Lord, Brian, Wang, Qi, Ao, Hong, Scott, Brian, Sepassi, Kia, Lovenberg, Timothy W., Carruthers, Nicholas I., Bhattacharya, Anindya, Letavic, Michael A.
Published in Journal of medicinal chemistry (22.09.2016)
Published in Journal of medicinal chemistry (22.09.2016)
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Journal Article
Comparison of aqueous solubility estimation from AQUAFAC and the GSE
Jain, Parijat, Sepassi, Kia, Yalkowsky, Samuel H.
Published in International journal of pharmaceutics (06.08.2008)
Published in International journal of pharmaceutics (06.08.2008)
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Simplified Estimation of the Octanol−Air Partition Coefficient
Sepassi, Kia, Yalkowsky, Samuel H
Published in Industrial & engineering chemistry research (28.03.2007)
Published in Industrial & engineering chemistry research (28.03.2007)
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Accounting for the Effects of Moderately Increased Pressure on the Energetics of Melting and Solubility in Metered Dose Inhalers: Innovative Inhalation Technologies
MOGALIAN, Erik, SEPASSI, Kia, MYRDAL, Paul Brian
Published in Drug development and industrial pharmacy (2008)
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Published in Drug development and industrial pharmacy (2008)
Journal Article
Estimating Pure-Component Vapor Pressures of Complex Organic Molecules: Part II
Sepassi, Kia, Myrdal, Paul B, Yalkowsky, Samuel H
Published in Industrial & engineering chemistry research (06.12.2006)
Published in Industrial & engineering chemistry research (06.12.2006)
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Journal Article
Pharmacological Characterization of 1-(5-Chloro-6-(trifluoromethoxy)-1 H -benzoimidazol-2-yl)-1 H -pyrazole-4-carboxylic Acid (JNJ-42041935), a Potent and Selective Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor
Barrett, Terrance D., Palomino, Heather L., Brondstetter, Theresa I., Kanelakis, Kimon C., Wu, Xiaodong, Haug, Peter V., Yan, Wen, Young, Andrew, Hua, Hong, Hart, Juliet C., Tran, Da-Thao, Venkatesan, Hariharan, Rosen, Mark D., Peltier, Hillary M., Sepassi, Kia, Rizzolio, Michele C., Bembenek, Scott D., Mirzadegan, Tara, Rabinowitz, Michael H., Shankley, Nigel P.
Published in Molecular pharmacology (01.06.2011)
Published in Molecular pharmacology (01.06.2011)
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Journal Article