3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma
Xu, Rui, Wang, Keshi, Rizzi, James P, Huang, Heli, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Wehn, Paul M, Yang, Hanbiao, Dixon, Darryl D, Czerwinski, Robert M, Du, Xinlin, Ged, Emily L, Han, Guangzhou, Tan, Huiling, Wong, Tai, Xie, Shanhai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
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A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma
Wallace, Eli M, Rizzi, James P, Han, Guangzhou, Wehn, Paul M, Cao, Zhaodan, Du, Xinlin, Cheng, Tzuling, Czerwinski, Robert M, Dixon, Darryl D, Goggin, Barry S, Grina, Jonas A, Halfmann, Megan M, Maddie, Melissa A, Olive, Sarah R, Schlachter, Stephen T, Tan, Huiling, Wang, Bin, Wang, Keshi, Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A
Published in Cancer research (Chicago, Ill.) (15.09.2016)
Published in Cancer research (Chicago, Ill.) (15.09.2016)
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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Journal Article
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Modulating fast skeletal muscle contraction protects skeletal muscle in animal models of Duchenne muscular dystrophy
Russell, Alan J, DuVall, Mike, Barthel, Ben, Qian, Ying, Peter, Angela K, Newell-Stamper, Breanne L, Hunt, Kevin, Lehman, Sarah, Madden, Molly, Schlachter, Stephen, Robertson, Ben, Van Deusen, Ashleigh, Rodriguez, Hector M, Vera, Carlos, Su, Yu, Claflin, Dennis R, Brooks, Susan V, Nghiem, Peter, Rutledge, Alexis, Juehne, Twlya I, Yu, Jinsheng, Barton, Elisabeth R, Luo, Yangyi E, Patsalos, Andreas, Nagy, Laszlo, Sweeney, H Lee, Leinwand, Leslie A, Koch, Kevin
Published in The Journal of clinical investigation (15.05.2023)
Published in The Journal of clinical investigation (15.05.2023)
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Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors
Blake, James F, Xu, Rui, Bencsik, Josef R, Xiao, Dengming, Kallan, Nicholas C, Schlachter, Stephen, Mitchell, Ian S, Spencer, Keith L, Banka, Anna L, Wallace, Eli M, Gloor, Susan L, Martinson, Matthew, Woessner, Richard D, Vigers, Guy P.A, Brandhuber, Barbara J, Liang, Jun, Safina, Brian S, Li, Jun, Zhang, Birong, Chabot, Christine, Do, Steven, Lee, Leslie, Oeh, Jason, Sampath, Deepak, Lee, Brian B, Lin, Kui, Liederer, Bianca M, Skelton, Nicholas J
Published in Journal of medicinal chemistry (27.09.2012)
Published in Journal of medicinal chemistry (27.09.2012)
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Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction
Wehn, Paul M., Yang, Song, Grina, Jonas A., Rizzi, James P., Schlachter, Stephen T., Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Czerwinski, Robert M., Ged, Emily L., Huang, Heli, Halfmann, Megan M., Maddie, Melissa A., Morton, Emily R., Olive, Sarah R., Tan, Huiling, Xie, Shanhai, Josey, John A., Wallace, Eli M.
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
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DNA-dependent protein kinase inhibitors as drug candidates for the treatment of cancer
Kashishian, Adam, Douangpanya, Heather, Clark, Darcey, Schlachter, Stephen T, Eary, C Todd, Schiro, Justin G, Huang, Hongmei, Burgess, Larry E, Kesicki, Edward A, Halbrook, James
Published in Molecular cancer therapeutics (01.12.2003)
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Published in Molecular cancer therapeutics (01.12.2003)
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Discovery of a Novel Class of Imidazo[1,2‑a]Pyridines with Potent PDGFR Activity and Oral Bioavailability
Hicken, Erik J, Marmsater, Fred P, Munson, Mark C, Schlachter, Stephen T, Robinson, John E, Allen, Shelley, Burgess, Laurence E, DeLisle, Robert Kirk, Rizzi, James P, Topalov, George T, Zhao, Qian, Hicks, Julie M, Kallan, Nicholas C, Tarlton, Eugene, Allen, Andrew, Callejo, Michele, Cox, April, Rana, Sumeet, Klopfenstein, Nathalie, Woessner, Richard, Lyssikatos, Joseph P
Published in ACS medicinal chemistry letters (09.01.2014)
Published in ACS medicinal chemistry letters (09.01.2014)
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Pyrimidine Thioethers: A Novel Class of HIV-1 Reverse Transcriptase Inhibitors with Activity Against BHAP-Resistant HIV
Nugent, Richard A, Schlachter, Stephen T, Murphy, Michael J, Cleek, Gary J, Poel, Toni J, Wishka, Donn G, Graber, David R, Yagi, Yoshihiko, Keiser, Barbara J, Olmsted, Robert A, Kopta, Laurie A, Swaney, Steven M, Poppe, Susan M, Morris, Joel, Tarpley, W. Gary, Thomas, Richard C
Published in Journal of medicinal chemistry (24.09.1998)
Published in Journal of medicinal chemistry (24.09.1998)
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EDG-002, A NOVEL TARGETED SARCOMERE REGULATOR PRESERVES INTRINSIC MYOSIN-MOTOR FUNCTION, BLUNTS HYPERCONTRACTILITY AND ELIMINATES LVOT OBSTRUCTION IN CATS WITH HYPERTROPHIC CARDIOMYOPATHY: IN VITRO AND IN VIVO EVIDENCE
Kaplan, Joanna, Lehman, Sarah, Duvall, Mike, Madden, Molly, Tolley, Jessica, Hawryluk, Natalie, Schlachter, Stephen, Rivas, Victor, Jauregui, Carina, Crofton, Amanda, Harris, Samantha, Stern, Joshua Aaron, del Rio, Carlos L., Russell, Alan, Evanchik, Marc
Published in Journal of the American College of Cardiology (07.03.2023)
Published in Journal of the American College of Cardiology (07.03.2023)
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피리다지논 화합물 및 이의 용도
SCHLACHTER STEPHEN, RUSSELL ALAN, WINSHIP PAUL, HUNT KEVIN, KOCH KEVIN, STEELE CHRIS, UZOHO GRACE
Year of Publication 17.08.2021
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Year of Publication 17.08.2021
Patent
피리다지논 화합물 및 이의 용도
SCHLACHTER STEPHEN, RUSSELL ALAN, WINSHIP PAUL, HUNT KEVIN, KOCH KEVIN, STEELE CHRIS
Year of Publication 13.08.2021
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Year of Publication 13.08.2021
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Pyrazoline bisphosphonate esters as novel antiinflammatory and antiarthritic agents
Nugent, Richard A., Murphy, Megan, Schlachter, Stephen T., Dunn, Colin J., Smith, Robert J., Staite, Nigel D., Galinet, Louise A., Shields, Sharon K., Aspar, Danielle G., Richard, Karen A., Rohloff, Norman A.
Published in Journal of medicinal chemistry (1993)
Published in Journal of medicinal chemistry (1993)
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Abstract B140: PT2977, a novel HIF-2a antagonist, has potent antitumor activity and remodels the immunosuppressive tumor microenvironment in clear cell renal cell cancer
Wong, Tai W., Shrimali, Rajeev, Contreras, Cristina, Cheng, Tzuling, Czerwinski, Robert M., Dixon, Daryl D., Du, Xinlin, Fett, Craig, Goree, Jessica, Grina, Jonas A., Han, Guangzhou, Huang, Heli, Rizzi, Jim, Schlachter, Stephen T., Wang, Bin, Wang, Keshi, Wehn, Paul M., Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A., Wallace, Eli M.
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Journal Article
Carbonyl-Containing Bisphosphonate Esters as Novel Antiinflammatory and Antiarthritic Agents
Nugent, Richard A, Schlachter, Stephen T, Murphy, Megan, Dunn, Colin J, Staite, Nigel D, Galinet, Louise A, Shields, Sharon K, Wu, Haiyan, Aspar, Danielle G, Richard, Karen A
Published in Journal of medicinal chemistry (01.12.1994)
Published in Journal of medicinal chemistry (01.12.1994)
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Abstract DDT01-01: PT2385: First-in-class HIF-2α antagonist for the treatment of renal cell carcinoma
Wallace, Eli M., Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert, Dixon, Darryl D., Du, Xinlin, Goggin, Barry, Grina, Jonas, Halfmann, Megan, Han, Guangzhou, Huang, Heli, Josey, John A., Maddie, Melissa A., Olive, Sarah, Rizzi, James, Schlachter, Stephen T., Tan, Hui-Ling, Wang, Bin, Wang, Keshi, Wehn, Paul M., Xie, Shanhai, Xu, Rui, Yang, Hanbiao
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Non-oxime inhibitors of B-Raf(V600E) kinase
Ren, Li, Wenglowsky, Steve, Miknis, Greg, Rast, Bryson, Buckmelter, Alex J, Ely, Robert J, Schlachter, Stephen, Laird, Ellen R, Randolph, Nikole, Callejo, Michele, Martinson, Matthew, Galbraith, Sarah, Brandhuber, Barbara J, Vigers, Guy, Morales, Tony, Voegtli, Walter C, Lyssikatos, Joseph
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
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The Discovery of furo[2,3- c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors
Buckmelter, Alex J., Ren, Li, Laird, Ellen R., Rast, Bryson, Miknis, Greg, Wenglowsky, Steve, Schlachter, Stephen, Welch, Mike, Tarlton, Eugene, Grina, Jonas, Lyssikatos, Joseph, Brandhuber, Barbara J., Morales, Tony, Randolph, Nikole, Vigers, Guy, Martinson, Matthew, Callejo, Michele
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
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Non-oxime inhibitors of B-Raf super(V600E) kinase
Ren, Li, Wenglowsky, Steve, Miknis, Greg, Rast, Bryson, Buckmelter, Alex J, Ely, Robert J, Schlachter, Stephen, Laird, Ellen R, Randolph, Nikole, Callejo, Michele, Martinson, Matthew, Galbraith, Sarah, Brandhuber, Barbara J, Vigers, Guy, Morales, Tony, Voegtli, Walter C, Lyssikatos, Joseph
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
Published in Bioorganic & medicinal chemistry letters (15.02.2011)
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