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-(diphenylme... von 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

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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 In... von 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

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Inhibition of Cytosolic Phospholipase A2α: Hit to Lead Optimization von 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

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Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α2α von 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

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Cytosolic phospholipase A2 alpha-deficient mice are resistant to experimental autoimmune encephalomyelitis von 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

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Blockade of cytosolic phospholipase A2 α prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses von 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

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Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α von 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

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Benzhydrylquinazolinediones: Novel cytosolic phospholipase A2α inhibitors with improved physicochemical properties von KIRINCICH, Steven J, JASON XIANG, GREEN, Neal, TAM, Steve, YANG, Hui Y, SHIM, Jaechul, SHEN, Marina W. H, CLARK, James D, MCKEW, John C

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Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A 2 α Inhibitors von 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.

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A fluorescence-based assay for fatty acid amide hydrolase compatible with high-throughput screening von Ramarao, Manjunath K., Murphy, Elizabeth A., Shen, Marina W.H., Wang, Yuren, Bushell, Kristen N., Huang, Nelson, Pan, Ning, Williams, Cara, Clark, James D.

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The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid von 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

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Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2α : Optimization of in vitro potency and rat pharmacokinetics for oral efficacy von 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

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Thermodynamic characterization of cytosolic phospholipase A2 alpha inhibitors von 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

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Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A2α Inhibitors von 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

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The cPLA sub(2) alpha inhibitor efipladib decreases nociceptive responses without affecting PGE sub(2) levels in the cerebral spinal fluid von Nickerson-Nutter, Cheryl L, Goodwin, Debra, Shen, Marina WH, Damphousse, Christy, Duan, Weili, Samad, Tarek A, McKew, John C, Lee, Katherine L, Zaleska, Margaret M, Mollova, Nevena, Clark, James D

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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-(diphenylm... von 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.

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Benzhydrylquinazolinediones: Novel cytosolic phospholipase A sub(2) alpha inhibitors with improved physicochemical properties von Kirincich, Steven J, Xiang, Jason, Green, Neal, Tam, Steve, Yang, Hui Y, Shim, Jaechul, Shen, Marina WH, Clark, James D, McKew, John C

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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)-l-(diphenylm... von MCKEW, John C, LEE, Katherine L, CHEN, Lihren, KIRINCICH, Steven J, MICHALAK, Ronald, THOMASON, Jennifer, IPEK, Manus, KUN WU, WOODER, Lane, RAMARAO, Manjunath K, MURPHY, Elizabeth A, GOODWIN, Debra G, SHEN, Marina W. H, ALBERT, Leo, XIN XU, DONAHUE, Frances, SHERRY KU, M, KEITH, James, NICKERSON-NUTTER, Cheryl L, ABRAHAM, William M, WILLIAMS, Cara, HEGEN, Martin, CLARK, James D, THAKKER, Paresh, FOLEY, Megan A, BEHNKE, Mark L, BAIHUA HU, SUM, Fuk-Wah, TAM, Steve, YONGHAN HU

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Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha von 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

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Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α 2 α von 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.

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