Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt)
Lugar, Charles W, Clarke, Christian A, Morphy, Richard, Rudyk, Helene, Sapmaz, Selma, Stites, Ryan E, Vaught, Grant M, Furness, Kelly, Broughton, Howard B, Durst, Greg L, Clawson, David K, Stout, Stephanie L, Guo, Sherry Y, Durbin, Jim D, Stayrook, Keith R, Edmondson, Denise D, Kikly, Kristy, New, Nicole E, Bina, Holly A, Chambers, Mark G, Shetler, Pamela, Chang, William Y, Chang, Veavi Ching-Yun, Barr, Rob, Gough, Wendy H, Steele, Jimmy P, Getman, Brian, Patel, Nita, Mathes, Brian M, Richardson, Timothy I
Published in Journal of medicinal chemistry (13.05.2021)
Published in Journal of medicinal chemistry (13.05.2021)
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Journal Article
Benzopyrans Are Selective Estrogen Receptor β Agonists with Novel Activity in Models of Benign Prostatic Hyperplasia
Norman, Bryan H, Dodge, Jeffrey A, Richardson, Timothy I, Borromeo, Peter S, Lugar, Charles W, Jones, Scott A, Chen, Keyue, Wang, Yong, Durst, Gregory L, Barr, Robert J, Montrose-Rafizadeh, Chahrzad, Osborne, Harold E, Amos, Robert M, Guo, Sherry, Boodhoo, Amechand, Krishnan, Venkatesh
Published in Journal of medicinal chemistry (19.10.2006)
Published in Journal of medicinal chemistry (19.10.2006)
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Journal Article
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids
Richardson, Timothy I, Clarke, Christian A, Yu, Kuo-Long, Yee, Ying K, Bleisch, Thomas J, Lopez, Jose E, Jones, Scott A, Hughes, Norman E, Muehl, Brian S, Lugar, Charles W, Moore, Terry L, Shetler, Pamela K, Zink, Richard W, Osborne, John J, Montrose-Rafizadeh, Chahrzad, Patel, Nita, Geiser, Andrew G, Galvin, Rachelle J. Sells, Dodge, Jeffrey A
Published in ACS medicinal chemistry letters (10.02.2011)
Published in ACS medicinal chemistry letters (10.02.2011)
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Journal Article
Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 2: Structure–activity relationship studies on the benzopyran scaffold
Richardson, Timothy I., Norman, Bryan H., Lugar, Charles W., Jones, Scott A., Wang, Yong, Durbin, Jim D., Krishnan, Venkatesh, Dodge, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (01.07.2007)
Published in Bioorganic & medicinal chemistry letters (01.07.2007)
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Journal Article
Structure−Activity Studies of 6-(Tetrazolylalkyl)-Substituted Decahydroisoquinoline-3-carboxylic Acid AMPA Receptor Antagonists. 1. Effects of Stereochemistry, Chain Length, and Chain Substitution
Ornstein, Paul L, Arnold, M. Brian, Allen, Nancy K, Bleisch, Thomas, Borromeo, Peter S, Lugar, Charles W, Leander, J. David, Lodge, David, Schoepp, Darryle D
Published in Journal of medicinal chemistry (24.05.1996)
Published in Journal of medicinal chemistry (24.05.1996)
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Journal Article
Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats
Lugar, Charles W., Clay, Michael P., Lindstrom, Terry D., Woodson, Andrea L., Smiley, David, Heiman, Mark L., Dodge, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (06.12.2004)
Published in Bioorganic & medicinal chemistry letters (06.12.2004)
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Journal Article
B-ring unsaturated estrogens: Biological evaluation of 17α-dihydroequilein and novel B-nor-6-thiaequilenins as tissue selective estrogens
LUGAR, Charles W, MAGEE, David, ADRIAN, Mary D, SHETLER, Pamela, BRYANT, Henry U, DODGE, Jeffrey A
Published in Bioorganic & medicinal chemistry letters (15.12.2003)
Published in Bioorganic & medicinal chemistry letters (15.12.2003)
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Journal Article
B-ring unsaturated estrogens: biological evaluation of 17alpha-Dihydroequilein and novel B-Nor-6-thiaequilenins as tissue selective estrogens
Lugar, 3rd, Charles W, Magee, David, Adrian, Mary D, Shetler, Pamela, Bryant, Henry U, Dodge, Jeffrey A
Published in Bioorganic & medicinal chemistry letters (15.12.2003)
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Published in Bioorganic & medicinal chemistry letters (15.12.2003)
Journal Article
Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity
Dodge, Jeffrey A., Lugar, Charles W., Cho, Stephen, Short, Lorri L., Sato, Masahiko, Yang, Na N., Spangle, Larry A., Martin, Michael J., Phillips, David L., Glasebrook, Andrew L., Osborne, John J., Frolik, Charles A., Bryant, Henry U.
Published in The Journal of steroid biochemistry and molecular biology (01.04.1997)
Published in The Journal of steroid biochemistry and molecular biology (01.04.1997)
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Journal Article
Structure−Activity Studies of 6-Substituted Decahydroisoquinoline-3-carboxylic Acid AMPA Receptor Antagonists. 2. Effects of Distal Acid Bioisosteric Substitution, Absolute Stereochemical Preferences, and in Vivo Activity
Ornstein, Paul L, Arnold, M. Brian, Allen, Nancy K, Bleisch, Thomas, Borromeo, Peter S, Lugar, Charles W, Leander, J. David, Lodge, David, Schoepp, Darryle D
Published in Journal of medicinal chemistry (24.05.1996)
Published in Journal of medicinal chemistry (24.05.1996)
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Journal Article
Development of analytical and preparative chromatographic separations of novel growth hormone secretagogue compounds
Kennedy, Joseph H, Bowers, John L, Dodge, Jeffrey A, Lugar, Charles W, Shepherd, Timothy A, Sharp, V.Scott
Published in Journal of Chromatography A (03.03.2000)
Published in Journal of Chromatography A (03.03.2000)
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Journal Article
Structure−Activity Relationships of Selective Estrogen Receptor Modulators: Modifications to the 2-Arylbenzothiophene Core of Raloxifene
Grese, Timothy A, Cho, Stephen, Finley, Don R, Godfrey, Alexander G, Jones, Charles D, Lugar, Charles W, Martin, Michael J, Matsumoto, Ken, Pennington, Lewis D, Winter, Mark A, Adrian, M. Dee, Cole, Harlan W, Magee, David E, Phillips, D. Lynn, Rowley, Ellen R, Short, Lorri L, Glasebrook, Andrew L, Bryant, Henry U
Published in Journal of medicinal chemistry (17.01.1997)
Published in Journal of medicinal chemistry (17.01.1997)
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Journal Article
cGAS INHIBITORS
AHMED, Adel, GERNERT, Douglas L, CARSON, Cheryl Ann, TROMICZAK, Eric George, LUGAR, Charles W, FORTNER, Kevin Charles, ONOBUN, Emmanuel, CUMMING, Graham Robert, AGEJAS CHICHARRO, Francisco Javier, NAGARAJAN, Shanthi, MARTINEZ BROKAW, Christina, VARIN, Thibault Francois, GREEN, Steven J, CONNER, Scott Eugene, MARIMUTHU, Jothirajah
Year of Publication 25.07.2024
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Year of Publication 25.07.2024
Patent
AZEPINO[4,5-B]INDOLONE CGAS INHIBITORS
AHMED, Adel, GERNERT, Douglas L, CARSON, Cheryl Ann, TROMICZAK, Eric George, LUGAR, Charles W, FORTNER, Kevin Charles, ONOBUN, Emmanuel, CUMMING, Graham Robert, AGEJAS CHICHARRO, Francisco Javier, NAGARAJAN, Shanthi, MARTINEZ BROKAW, Christina, VARIN, Thibault Francois, GREEN, Steven J, CONNER, Scott Eugene, MARIMUTHU, Jothirajah
Year of Publication 27.06.2024
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Year of Publication 27.06.2024
Patent
Solid-phase synthesis of unnatural amino acids using unactivated alkyl halides
O'Donnell, Martin J., Lugar, Charles W., Pottorf, Richard S., Zhou, Changyou, Scott, William L., Cwi, Cynthia L.
Published in Tetrahedron letters (13.10.1997)
Published in Tetrahedron letters (13.10.1997)
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Journal Article
Alcohol inversion of 17β-steroids
Dodge, Jeffrey A., Lugar, Charles W.
Published in Bioorganic & medicinal chemistry letters (09.01.1996)
Published in Bioorganic & medicinal chemistry letters (09.01.1996)
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Journal Article
CGAS INHIBITORS
CONNER, Scott E, AHMED, Adel, GERNERT, Douglas L, NICOLAOU, Christodoulos, CARSON, Cheryl Ann, LUGAR, Charles W. III, FRANCISKOVICH, Jeffry B, FORTNER, Kevin Charles, ONOBUN, Emmanuel, STOUT, Stephanie Lange, NAGARAJAN, Shanthi, VARIN, Thibault, MARTINEZ BROKAW, Christina, GREEN, Steven J, TROMICZAK, Eric G, MARIMUTHU, Jothirajah
Year of Publication 07.12.2023
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Year of Publication 07.12.2023
Patent
cGAS inhibitors
NAGARAJAN, SHANTHI, FORTNER, KEVIN CHARLES, ONOBUN, EMMANUEL, GERNERT, DOUGLAS L, NICOLAOU, CHRISTODOULOS, MARTINEZ BROKAW, CHRISTINA, AHMED, ADEL, TROMICZAK, ERIC G, FRANCISKOVICH, JEFFRY B, VARIN, THIBAULT, CARSON, CHERYL ANN, STOUT, STEPHANIE LANGE, LUGAR, CHARLES W, MARIMUTHU, JOTHIRAJAH, CONNER, SCOTT E, GREEN, STEVEN J
Year of Publication 01.05.2024
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Year of Publication 01.05.2024
Patent
Synthesis and estrogen receptor binding affinities of the major human metabolites of raloxifene (LY139481)
Dodge, Jeffrey A., Lugar, Charles W., Cho, Stephen, Osborne, John J., Phillips, David L., Glasebrook, Andrew L., Frolik, Charles A.
Published in Bioorganic & medicinal chemistry letters (22.04.1997)
Published in Bioorganic & medicinal chemistry letters (22.04.1997)
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Journal Article
cGAS INHIBITORS
CONNER, Scott E, AHMED, Adel, GERNERT, Douglas L, NICOLAOU, Christodoulos, CARSON, Cheryl Ann, FRANCISKOVICH, Jeffry B, FORTNER, Kevin Charles, ONOBUN, Emmanuel, STOUT, Stephanie Lange, LUGAR, III, Charles W, NAGARAJAN, Shanthi, VARIN, Thibault, MARTINEZ BROKAW, Christina, GREEN, Steven J, TROMICZAK, Eric G, MARIMUTHU, Jothirajah
Year of Publication 07.12.2023
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Year of Publication 07.12.2023
Patent