Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation
Arhancet, Graciela B., Walker, Daniel P., Metz, Sue, Fobian, Yvette M., Heasley, Steven E., Carter, Jeffrey S., Springer, John R., Jones, Darin E., Hayes, Michael J., Shaffer, Alexander F., Jerome, Gina M., Baratta, Michael T., Zweifel, Ben, Moore, William M., Masferrer, Jaime L., Vazquez, Michael L.
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
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Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor
Mbalaviele, Gabriel, Pauley, Adele M., Shaffer, Alexander F., Zweifel, Ben S., Mathialagan, Sumathy, Mnich, Stephen J., Nemirovskiy, Olga V., Carter, Jeff, Gierse, James K., Wang, Jane L., Vazquez, Michael L., Moore, William M., Masferrer, Jaime L.
Published in Biochemical pharmacology (15.05.2010)
Published in Biochemical pharmacology (15.05.2010)
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Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase
Graneto, Matthew J, Kurumbail, Ravi G, Vazquez, Michael L, Shieh, Huey-Sheng, Pawlitz, Jennifer L, Williams, Jennifer M, Stallings, William C, Geng, Lifeng, Naraian, Ashok S, Koszyk, Francis J, Stealey, Michael A, Xu, Xiangdong D, Weier, Richard M, Hanson, Gunnar J, Mourey, Robert J, Compton, Robert P, Mnich, Stephen J, Anderson, Gary D, Monahan, Joseph B, Devraj, Rajesh
Published in Journal of medicinal chemistry (15.11.2007)
Published in Journal of medicinal chemistry (15.11.2007)
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
Vazquez, Michael L, Kaila, Neelu, Strohbach, Joseph W, Trzupek, John D, Brown, Matthew F, Flanagan, Mark E, Mitton-Fry, Mark J, Johnson, Timothy A, TenBrink, Ruth E, Arnold, Eric P, Basak, Arindrajit, Heasley, Steven E, Kwon, Soojin, Langille, Jonathan, Parikh, Mihir D, Griffin, Sarah H, Casavant, Jeffrey M, Duclos, Brian A, Fenwick, Ashley E, Harris, Thomas M, Han, Seungil, Caspers, Nicole, Dowty, Martin E, Yang, Xin, Banker, Mary Ellen, Hegen, Martin, Symanowicz, Peter T, Li, Li, Wang, Lu, Lin, Tsung H, Jussif, Jason, Clark, James D, Telliez, Jean-Baptiste, Robinson, Ralph P, Unwalla, Ray
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Evaluation of a Janus kinase 1 inhibitor, PF‐04965842, in healthy subjects: A phase 1, randomized, placebo‐controlled, dose‐escalation study
Peeva, Elena, Hodge, Martin R., Kieras, Elizabeth, Vazquez, Michael L., Goteti, Kosalaram, Tarabar, Sanela G., Alvey, Christine W., Banfield, Christopher
Published in British journal of clinical pharmacology (01.08.2018)
Published in British journal of clinical pharmacology (01.08.2018)
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Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists
Schnute, Mark E., Trujillo, John I., Lee, Katherine L., Unwalla, Ray, Vajdos, Felix F., Kauppi, Björn, Nuhant, Philippe, Flick, Andrew C., Crouse, Kimberly K., Zhao, Yajuan, Samuel, Amanda, Lombardo, Vincent, Taylor, Alexandria P., Brault, Amy L., Knafels, John D., Vazquez, Michael L., Berstein, Gabriel
Published in ACS medicinal chemistry letters (09.02.2023)
Published in ACS medicinal chemistry letters (09.02.2023)
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Novel benzoxazole inhibitors of mPGES-1
Kablaoui, Natasha, Patel, Snahel, Shao, Jay, Demian, Douglas, Hoffmaster, Keith, Berlioz, Francioise, Vazquez, Michael L., Moore, William M., Nugent, Richard A.
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
Published in Bioorganic & medicinal chemistry letters (01.02.2013)
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Renal effects induced by prolonged mPGES1 inhibition
Salazar, Francisco, Vazquez, Michael L, Masferrer, Jaime L, Mbalaviele, Gabriel, Llinas, Maria T, Saez, Fara, Arhancet, Grace, Salazar, F Javier
Published in American journal of physiology. Renal physiology (01.01.2014)
Published in American journal of physiology. Renal physiology (01.01.2014)
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Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: Use of a conformation-based hypothesis to facilitate compound design
Walker, Daniel P., Arhancet, Graciela B., Lu, Hwang-Fun, Heasley, Steven E., Metz, Sue, Kablaoui, Natasha M., Franco, Francisco M., Hanau, Cathleen E., Scholten, Jeffrey A., Springer, John R., Fobian, Yvette M., Carter, Jeffrey S., Xing, Li, Yang, Shengtian, Shaffer, Alexander F., Jerome, Gina M., Baratta, Michael T., Moore, William M., Vazquez, Michael L.
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
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Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system
Caspers, Nicole L., Han, Seungil, Rajamohan, Francis, Hoth, Lise R., Geoghegan, Kieran F., Subashi, Timothy A., Vazquez, Michael L., Kaila, Neelu, Cronin, Ciarán N., Johnson, Eric, Kurumbail, Ravi G.
Published in Acta crystallographica. Section F, Structural biology communications (01.11.2016)
Published in Acta crystallographica. Section F, Structural biology communications (01.11.2016)
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A Practical Synthesis of [(1S,3S)-3-Aminocyclohexyl]methanol and 2-[(1S,3S)-3-Aminocyclohexyl]propan-2-ol, Useful Intermediates for the Preparation of Novel mPGES-1 Inhibitors
Walker, Daniel P., Heasley, Steven E., MacInnes, Allison, Anjeh, Tizah, Lu, Hwang-Fun, Fobian, Yvette M., Collins, Joe T., Vazquez, Michael L., Mao, Michael K.
Published in Synlett (01.12.2011)
Published in Synlett (01.12.2011)
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Homo-timeric structural model of human microsomal prostaglandin E synthase-1 and characterization of its substrate/inhibitor binding interactions
Xing, Li, Kurumbail, Ravi G., Frazier, Ronald B., Davies, Michael S., Fujiwara, Hideji, Weinberg, Robin A., Gierse, James K., Caspers, Nicole, Carter, Jeffrey S., McDonald, Joseph J., Moore, William M., Vazquez, Michael L.
Published in Journal of computer-aided molecular design (2009)
Published in Journal of computer-aided molecular design (2009)
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Benzodipyrazoles: a new class of potent CDK2 inhibitors
D’Alessio, Roberto, Bargiotti, Alberto, Metz, Suzanne, Brasca, M. Gabriella, Cameron, Alexander, Ermoli, Antonella, Marsiglio, Aurelio, Polucci, Paolo, Roletto, Fulvia, Tibolla, Marcellino, Vazquez, Michael L., Vulpetti, Anna, Pevarello, Paolo
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
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RORC2 - - METHYL- AND TRIFLUOROMETHYL-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF
ZAMARATSKI EDOUARD, JONES PETER, WENNERSTAL GORAN MATTIAS, MENTE SCOT RICHARD, KAILA NEELU, ZHANG LIYING, TRZUPEK JOHN DAVID, VAZQUEZ MICHAEL L, SCHNUTE MARK EDWARD, FLICK ANDREW CHRISTOPHER, XING LI
Year of Publication 25.04.2017
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Year of Publication 25.04.2017
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Hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
JOHN J TALLEY JOHN J TALLEY, JOHN N FRESKOS JOHN N FRESKOS, MICHAEL L VAZQUEZ MICHAEL L VAZQUEZ, GARY A DECRESCENZO GARY A DECRESCENZO, RICHARD A. MUELLER RICHARD A. MUELLER, DANIEL GETMAN DANIEL GETMAN
Year of Publication 17.05.2007
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Year of Publication 17.05.2007
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PYRROLO [2,3-D]PYRIMIDINE DERIVATIVES AS INHIBITORS OF JANUS-RELATED KINASES (JAK)
UNWALLA RAYOMAND JAL, GONZALES ANDREA, JOHNSON TIMOTHY ALLAN, STROHBACH JOSEPH WALTER, TRZUPEK JOHN DAVID, TENBRINK RUTH E, MITTON FRY MARK J, FLANAGAN MARK EDWARD, KAILA NEELU, BROWN MATTHEW FRANK, FENWICK ASHLEY EDWARD, VAZQUEZ MICHAEL L, PARIKH MIHIR D
Year of Publication 01.10.2015
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Year of Publication 01.10.2015
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Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere
Getman, Daniel P, DeCrescenzo, Gary A, Heintz, Robert M, Reed, Kathryn L, Talley, John J, Bryant, Martin L, Clare, Michael, Houseman, Kathryn A, Marr, J. Joseph
Published in Journal of medicinal chemistry (1993)
Published in Journal of medicinal chemistry (1993)
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Pyrrolo[2,3-d]pyrimidine derivatives
Verhoest, Patrick Robert, Reese, Matthew R, Samad, Tarek, Vazquez, Michael L, Kaila, Neelu, Tuttle, Jamison B, Parikh, Mihir D, Coffman, Karen J, Duerr, James M, Sciabola, Simone
Year of Publication 06.04.2021
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Year of Publication 06.04.2021
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