Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic Acid, Efipladib
McKew, John C, Lee, Katherine L, Shen, Marina W. H, Thakker, Paresh, Foley, Megan A, Behnke, Mark L, Hu, Baihua, Sum, Fuk-Wah, Tam, Steve, Hu, Yonghan, Chen, Lihren, Kirincich, Steven J, Michalak, Ronald, Thomason, Jennifer, Ipek, Manus, Wu, Kun, Wooder, Lane, Ramarao, Manjunath K, Murphy, Elizabeth A, Goodwin, Debra G, Albert, Leo, Xu, Xin, Donahue, Frances, Ku, M. Sherry, Keith, James, Nickerson-Nutter, Cheryl L, Abraham, William M, Williams, Cara, Hegen, Martin, Clark, James D
Published in Journal of medicinal chemistry (26.06.2008)
Published in Journal of medicinal chemistry (26.06.2008)
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Discovery of Clinical Candidate 1‑{[(2S,3S,4S)‑3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design
Lee, Katherine L, Ambler, Catherine M, Anderson, David R, Boscoe, Brian P, Bree, Andrea G, Brodfuehrer, Joanne I, Chang, Jeanne S, Choi, Chulho, Chung, Seungwon, Curran, Kevin J, Day, Jacqueline E, Dehnhardt, Christoph M, Dower, Ken, Drozda, Susan E, Frisbie, Richard K, Gavrin, Lori K, Goldberg, Joel A, Han, Seungil, Hegen, Martin, Hepworth, David, Hope, Heidi R, Kamtekar, Satwik, Kilty, Iain C, Lee, Arthur, Lin, Lih-Ling, Lovering, Frank E, Lowe, Michael D, Mathias, John P, Morgan, Heidi M, Murphy, Elizabeth A, Papaioannou, Nikolaos, Patny, Akshay, Pierce, Betsy S, Rao, Vikram R, Saiah, Eddine, Samardjiev, Ivan J, Samas, Brian M, Shen, Marina W. H, Shin, Julia H, Soutter, Holly H, Strohbach, Joseph W, Symanowicz, Peter T, Thomason, Jennifer R, Trzupek, John D, Vargas, Richard, Vincent, Fabien, Yan, Jiangli, Zapf, Christoph W, Wright, Stephen W
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
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Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α2α
Lee, Katherine L, Foley, Megan A, Chen, Lihren, Behnke, Mark L, Lovering, Frank E, Kirincich, Steven J, Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W. H, Khor, SooPeang, Xu, Xin, Goodwin, Debra G, Ramarao, Manjunath K, Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M. Sherry, Clark, James D, McKew, John C
Published in Journal of medicinal chemistry (22.03.2007)
Published in Journal of medicinal chemistry (22.03.2007)
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Inhibition of Cytosolic Phospholipase A2α: Hit to Lead Optimization
McKew, John C, Foley, Megan A, Thakker, Paresh, Behnke, Mark L, Lovering, Frank E, Sum, Fuk-Wah, Tam, Steve, Wu, Kun, Shen, Marina W. H, Zhang, Wen, Gonzalez, Mario, Liu, Shanghao, Mahadevan, Anu, Sard, Howard, Khor, Soo Peang, Clark, James D
Published in Journal of medicinal chemistry (12.01.2006)
Published in Journal of medicinal chemistry (12.01.2006)
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Indole cytosolic phospholipase A(2) alpha inhibitors: Discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib
McKew, John C., Lee, Katherine L., Shen, Marina W. H., Thakker, Paresh, Foley, Megan A., Behnke, Mark L., Hu, Baihua, Sum, Fuk-Wah, Tam, Steve, Hu, Yonghan, Chen, Lihren, Kirincich, Steven J., Michalak, Ronald, Thomason, Jennifer, Ipek, Manus, Wu, Kun, Wooder, Lane, Ramarao, Manjunath K., Murphy, Elizabeth A., Goodwin, Debra G., Albert, Leo, Xu, Xin, Donahue, Frances, Ku, M. Sherry, Keith, James, Nickerson-Nutter, Cheryl L., Abraham, William M., Williams, Cara, Hegen, Martin, Clark, James D.
Published in Journal of medicinal chemistry (26.06.2008)
Published in Journal of medicinal chemistry (26.06.2008)
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Journal Article
Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A(2)alpha
Lee, Katherine L., Foley, Megan A., Chen, Lihren, Behnke, Mark L., Lovering, Frank E., Kirincich, Steven J., Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W. H., Khor, SooPeang, Xu, Xin, Goodwin, Debra G., Ramarao, Manjunath K., Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M. Sherry, Clark, James D., McKew, John C.
Published in Journal of medicinal chemistry (22.03.2007)
Published in Journal of medicinal chemistry (22.03.2007)
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Cytosolic phospholipase A2 alpha-deficient mice are resistant to experimental autoimmune encephalomyelitis
Marusic, Suzana, Leach, Michael W, Pelker, Jeffrey W, Azoitei, Mihai L, Uozumi, Naonori, Cui, Junqing, Shen, Marina W H, DeClercq, Charlene M, Miyashiro, Joy S, Carito, Brenda A, Thakker, Paresh, Simmons, David L, Leonard, John P, Shimizu, Takao, Clark, James D
Published in The Journal of experimental medicine (19.09.2005)
Published in The Journal of experimental medicine (19.09.2005)
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Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α
LEE, Katherine L, FOLEY, Megan A, KHOR, Soopeang, XIN XU, GOODWIN, Debra G, RAMARAO, Manjunath K, NICKERSON-NUTTER, Cheryl, DONAHUE, Frances, SHERRY KU, M, DARK, James D, MCKEW, John C, CHEN, Lihren, BEHNKE, Mark L, LOVERING, Frank E, KIRINCICH, Steven J, WEIHENG WANG, SHIM, Jaechul, TAM, Steve, SHEN, Marina W. H
Published in Journal of medicinal chemistry (22.03.2007)
Published in Journal of medicinal chemistry (22.03.2007)
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Blockade of cytosolic phospholipase A2 α prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses
Marusic, Suzana, Thakker, Paresh, Pelker, Jeffrey W, Stedman, Nancy L, Lee, Katherine L, McKew, John C, Han, Lixin, Xu, Xin, Wolf, Stan F, Borey, Adam J, Cui, Junqing, Shen, Marina W.H, Donahue, Fran, Hassan-Zahraee, Mina, Leach, Michael W, Shimizu, Takao, Clark, James D
Published in Journal of neuroimmunology (15.11.2008)
Published in Journal of neuroimmunology (15.11.2008)
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Benzhydrylquinazolinediones: Novel cytosolic phospholipase A2α inhibitors with improved physicochemical properties
KIRINCICH, Steven J, JASON XIANG, GREEN, Neal, TAM, Steve, YANG, Hui Y, SHIM, Jaechul, SHEN, Marina W. H, CLARK, James D, MCKEW, John C
Published in Bioorganic & medicinal chemistry (01.07.2009)
Published in Bioorganic & medicinal chemistry (01.07.2009)
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Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A(2)alpha Inhibitors
Chen, Lihren, Wang, Weiheng, Lee, Katherine L., Shen, Marina W. H., Murphy, Elizabeth A., Zhang, Wen, Xu, Xin, Tam, Steve, Nickerson-Nutter, Cheryl, Goodwin, Debra G., Clark, James D., McKew, John C.
Published in Journal of medicinal chemistry (26.02.2009)
Published in Journal of medicinal chemistry (26.02.2009)
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Journal Article
Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A 2 α Inhibitors
Chen, Lihren, Wang, Weiheng, Lee, Katherine L., Shen, Marina W. H., Murphy, Elizabeth A., Zhang, Wen, Xu, Xin, Tam, Steve, Nickerson-Nutter, Cheryl, Goodwin, Debra G., Clark, James D., McKew, John C.
Published in Journal of medicinal chemistry (26.02.2009)
Published in Journal of medicinal chemistry (26.02.2009)
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A fluorescence-based assay for fatty acid amide hydrolase compatible with high-throughput screening
Ramarao, Manjunath K., Murphy, Elizabeth A., Shen, Marina W.H., Wang, Yuren, Bushell, Kristen N., Huang, Nelson, Pan, Ning, Williams, Cara, Clark, James D.
Published in Analytical biochemistry (01.08.2005)
Published in Analytical biochemistry (01.08.2005)
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The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid
Nickerson-Nutter, Cheryl L, Goodwin, Debra, Shen, Marina W H, Damphousse, Christy, Duan, Weili, Samad, Tarek A, McKew, John C, Lee, Katherine L, Zaleska, Margaret M, Mollova, Nevena, Clark, James D
Published in Neuropharmacology (01.03.2011)
Published in Neuropharmacology (01.03.2011)
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Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2α : Optimization of in vitro potency and rat pharmacokinetics for oral efficacy
LEE, Katherine L, BEHNKE, Mark L, SHEN, Marina W. H, RAMARAO, Manjunath K, GOODWIN, Debra G, NICKERSON-NUTTER, Cheryl L, ABRAHAM, William M, WILLIAMS, Cara, CLARK, James D, MCKEW, John C, FOLEY, Megan A, CHEN, Lihren, WEIHENG WANG, VARGAS, Richard, NUNEZ, Jill, TAM, Steve, MOLLOVA, Nevena, XIN XU
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
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Journal Article
Thermodynamic characterization of cytosolic phospholipase A2 alpha inhibitors
Ramarao, Manjunath K, Shen, Marina W H, Murphy, Elizabeth A, Duan, Weili, Zhao, Yajuan, McKew, John, Lee, Katherine L, Thakker, Paresh, Behnke, Mark L, Clark, James D
Published in Analytical biochemistry (15.12.2008)
Published in Analytical biochemistry (15.12.2008)
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Journal Article
Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A2α Inhibitors
Chen, Lihren, Wang, Weiheng, Lee, Katherine L, Shen, Marina W. H, Murphy, Elizabeth A, Zhang, Wen, Xu, Xin, Tam, Steve, Nickerson-Nutter, Cheryl, Goodwin, Debra G, Clark, James D, McKew, John C
Published in Journal of medicinal chemistry (26.02.2009)
Published in Journal of medicinal chemistry (26.02.2009)
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Journal Article
Indole Cytosolic Phospholipase A 2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1 H -indol-3-yl]propyl}benzoic Acid, Efipladib
McKew, John C., Lee, Katherine L., Shen, Marina W. H., Thakker, Paresh, Foley, Megan A., Behnke, Mark L., Hu, Baihua, Sum, Fuk-Wah, Tam, Steve, Hu, Yonghan, Chen, Lihren, Kirincich, Steven J., Michalak, Ronald, Thomason, Jennifer, Ipek, Manus, Wu, Kun, Wooder, Lane, Ramarao, Manjunath K., Murphy, Elizabeth A., Goodwin, Debra G., Albert, Leo, Xu, Xin, Donahue, Frances, Ku, M. Sherry, Keith, James, Nickerson-Nutter, Cheryl L., Abraham, William M., Williams, Cara, Hegen, Martin, Clark, James D.
Published in Journal of medicinal chemistry (01.06.2008)
Published in Journal of medicinal chemistry (01.06.2008)
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Journal Article
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha
Lee, Katherine L, Foley, Megan A, Chen, Lihren, Behnke, Mark L, Lovering, Frank E, Kirincich, Steven J, Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W H, Khor, Soopeang, Xu, Xin, Goodwin, Debra G, Ramarao, Manjunath K, Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M Sherry, Clark, James D, McKew, John C
Published in Journal of medicinal chemistry (22.03.2007)
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Published in Journal of medicinal chemistry (22.03.2007)
Journal Article
Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α 2 α
Lee, Katherine L., Foley, Megan A., Chen, Lihren, Behnke, Mark L., Lovering, Frank E., Kirincich, Steven J., Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W. H., Khor, SooPeang, Xu, Xin, Goodwin, Debra G., Ramarao, Manjunath K., Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M. Sherry, Clark, James D., McKew, John C.
Published in Journal of medicinal chemistry (01.03.2007)
Published in Journal of medicinal chemistry (01.03.2007)
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