Identification of 4‑(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2)
Rowbottom, Martin W, Bain, Gretchen, Calderon, Imelda, Lasof, Taylor, Lonergan, David, Lai, Andiliy, Huang, Fei, Darlington, Janice, Prodanovich, Patricia, Santini, Angelina M, King, Christopher D, Goulet, Lance, Shannon, Kristen E, Ma, Gina L, Nguyen, Katherine, MacKenna, Deidre A, Evans, Jilly F, Hutchinson, John H
Published in Journal of medicinal chemistry (25.05.2017)
Published in Journal of medicinal chemistry (25.05.2017)
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Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor
Chao, Qi, Sprankle, Kelly G, Grotzfeld, Robert M, Lai, Andiliy G, Carter, Todd A, Velasco, Anne Marie, Gunawardane, Ruwanthi N, Cramer, Merryl D, Gardner, Michael F, James, Joyce, Zarrinkar, Patrick P, Patel, Hitesh K, Bhagwat, Shripad S
Published in Journal of medicinal chemistry (10.12.2009)
Published in Journal of medicinal chemistry (10.12.2009)
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Journal Article
Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis
Bain, Gretchen, Shannon, Kristen E, Huang, Fei, Darlington, Janice, Goulet, Lance, Prodanovich, Patricia, Ma, Gina L, Santini, Angelina M, Stein, Adam J, Lonergan, Dave, King, Christopher D, Calderon, Imelda, Lai, Andiliy, Hutchinson, John H, Evans, Jilly F
Published in The Journal of pharmacology and experimental therapeutics (01.01.2017)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2017)
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A small molecule-kinase interaction map for clinical kinase inhibitors
Zarrinkar, Patrick P, Floyd, Mark, Lai, Andiliy G, Atteridge, Corey E, Carter, Todd A, Galvin, Margaret, Mehta, Shamal A, Lélias, Jean-Michel, Wodicka, Lisa M, Benedetti, Michael G, Azimioara, Mihai D, Treiber, Daniel K, Insko, Darren E, Insko, Michael A, Edeen, Philip T, Gerlach, Jay L, Fabian, Miles A, Grotzfeld, Robert M, Lockhart, David J, Patel, Hitesh K, Milanov, Zdravko V, Ciceri, Pietro, Biggs, William H, Herrgard, Sanna, Velasco, Anne Marie, Ford, Julia M
Published in Nature biotechnology (01.03.2005)
Published in Nature biotechnology (01.03.2005)
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Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft
Govek, Steven P., Nagasawa, Johnny Y., Douglas, Karensa L., Lai, Andiliy G., Kahraman, Mehmet, Bonnefous, Celine, Aparicio, Anna M., Darimont, Beatrice D., Grillot, Katherine L., Joseph, James D., Kaufman, Joshua A., Lee, Kyoung-Jin, Lu, Nhin, Moon, Michael J., Prudente, Rene Y., Sensintaffar, John, Rix, Peter J., Hager, Jeffrey H., Smith, Nicholas D.
Published in Bioorganic & medicinal chemistry letters (15.11.2015)
Published in Bioorganic & medicinal chemistry letters (15.11.2015)
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Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E
Rowbottom, Martin W, Faraoni, Raffaella, Chao, Qi, Campbell, Brian T, Lai, Andiliy G, Setti, Eduardo, Ezawa, Maiko, Sprankle, Kelly G, Abraham, Sunny, Tran, Lan, Struss, Brian, Gibney, Michael, Armstrong, Robert C, Gunawardane, Ruwanthi N, Nepomuceno, Ronald R, Valenta, Ianina, Hua, Helen, Gardner, Michael F, Cramer, Merryl D, Gitnick, Dana, Insko, Darren E, Apuy, Julius L, Jones-Bolin, Susan, Ghose, Arup K, Herbertz, Torsten, Ator, Mark A, Dorsey, Bruce D, Ruggeri, Bruce, Williams, Michael, Bhagwat, Shripad, James, Joyce, Holladay, Mark W
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft
Govek, Steven P., Bonnefous, Celine, Julien, Jackaline D., Nagasawa, Johnny Y., Kahraman, Mehmet, Lai, Andiliy G., Douglas, Karensa L., Aparicio, Anna M., Darimont, Beatrice D., Grillot, Katherine L., Joseph, James D., Kaufman, Joshua A., Lee, Kyoung-Jin, Lu, Nhin, Moon, Michael J., Prudente, Rene Y., Sensintaffar, John, Rix, Peter J., Hager, Jeffrey H., Smith, Nicholas D.
Published in Bioorganic & medicinal chemistry letters (01.02.2019)
Published in Bioorganic & medicinal chemistry letters (01.02.2019)
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Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors
Patel, Hitesh K., Grotzfeld, Robert M., Lai, Andiliy G., Mehta, Shamal A., Milanov, Zdravko V., Chao, Qi, Sprankle, Kelly G., Carter, Todd A., Velasco, Anne Marie, Fabian, Miles A., James, Joyce, Treiber, Daniel K., Lockhart, David J., Zarrinkar, Patrick P., Bhagwat, Shripad S.
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
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Journal Article
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors
Holladay, Mark W., Campbell, Brian T., Rowbottom, Martin W., Chao, Qi, Sprankle, Kelly G., Lai, Andiliy G., Abraham, Sunny, Setti, Eduardo, Faraoni, Raffaella, Tran, Lan, Armstrong, Robert C., Gunawardane, Ruwanthi N., Gardner, Michael F., Cramer, Merryl D., Gitnick, Dana, Ator, Mark A., Dorsey, Bruce D., Ruggeri, Bruce R., Williams, Michael, Bhagwat, Shripad S., James, Joyce
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts
Lai, Andiliy, Kahraman, Mehmet, Govek, Steven, Nagasawa, Johnny, Bonnefous, Celine, Julien, Jackie, Douglas, Karensa, Sensintaffar, John, Lu, Nhin, Lee, Kyoung-jin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Moon, Michael J, Joseph, James D, Darimont, Beatrice, Brigham, Daniel, Grillot, Kate, Heyman, Richard, Rix, Peter J, Hager, Jeffrey H, Smith, Nicholas D
Published in Journal of medicinal chemistry (25.06.2015)
Published in Journal of medicinal chemistry (25.06.2015)
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Journal Article
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer
Nagasawa, Johnny, Govek, Steven, Kahraman, Mehmet, Lai, Andiliy, Bonnefous, Celine, Douglas, Karensa, Sensintaffar, John, Lu, Nhin, Lee, KyoungJin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Joseph, James D, Darimont, Beatrice, Brigham, Daniel, Maheu, Kate, Heyman, Richard, Rix, Peter J, Hager, Jeffrey H, Smith, Nicholas D
Published in Journal of medicinal chemistry (13.09.2018)
Published in Journal of medicinal chemistry (13.09.2018)
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Journal Article
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer
Joseph, James D, Darimont, Beatrice, Zhou, Wei, Arrazate, Alfonso, Young, Amy, Ingalla, Ellen, Walter, Kimberly, Blake, Robert A, Nonomiya, Jim, Guan, Zhengyu, Kategaya, Lorna, Govek, Steven P, Lai, Andiliy G, Kahraman, Mehmet, Brigham, Dan, Sensintaffar, John, Lu, Nhin, Shao, Gang, Qian, Jing, Grillot, Kate, Moon, Michael, Prudente, Rene, Bischoff, Eric, Lee, Kyoung-Jin, Bonnefous, Celine, Douglas, Karensa L, Julien, Jackaline D, Nagasawa, Johnny Y, Aparicio, Anna, Kaufman, Josh, Haley, Benjamin, Giltnane, Jennifer M, Wertz, Ingrid E, Lackner, Mark R, Nannini, Michelle A, Sampath, Deepak, Schwarz, Luis, Manning, Henry Charles, Tantawy, Mohammed Noor, Arteaga, Carlos L, Heyman, Richard A, Rix, Peter J, Friedman, Lori, Smith, Nicholas D, Metcalfe, Ciara, Hager, Jeffrey H
Published in eLife (13.07.2016)
Published in eLife (13.07.2016)
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Journal Article
Maximizing ER‑α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927
Kahraman, Mehmet, Govek, Steven P, Nagasawa, Johnny Y, Lai, Andiliy, Bonnefous, Celine, Douglas, Karensa, Sensintaffar, John, Liu, Nhin, Lee, KyoungJin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Joseph, James D, Darimont, Beatrice, Brigham, Daniel, Heyman, Richard, Rix, Peter J, Hager, Jeffrey H, Smith, Nicholas D
Published in ACS medicinal chemistry letters (10.01.2019)
Published in ACS medicinal chemistry letters (10.01.2019)
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HSD17B13 억제제 및 이의 용도
LAI ANDILIY G, GOVEK STEVEN P, HUDSON ANDREW R, FASANYA KARENSA L, SMITH NICHOLAS D
Year of Publication 18.07.2023
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Year of Publication 18.07.2023
Patent
Abstract 1648: Discovery and evolution of orally bioavailable selective estrogen receptor degraders for ER+ breast cancer: From GDC-0810 to GDC-0927
Kahraman, Mehmet, Govek, Steven P., Nagasawa, Johnny Y., Lai, Andiliy, Bonnefous, Celine, Douglas, Karensa, Sensintaffar, John, Lu, Nhin, Lee, KyoungJin, Aparicio, Anna, Kaufman, Josh, Qian, Jing, Shao, Gang, Prudente, Rene, Joseph, James D., Darimont, Beatrice, Brigham, Daniel, Heyman, Richard, Rix, Peter J., Hager, Jeffrey H., Smith, Nicholas D., Blake, Robert A., Chang, Jae, Choo, Edna, Daemen, Anneleen, Friedman, Lori S., Guan, Jane, Hartman, Steven, Ingalla, Ellen, Kiefer, James R., Kleinheinz, Tracy, Labadie, Sharada, Metcalfe, Ciara, Mody, Vidhi, Nannini, Michelle, Sampath, Deepak, Young, Amy, Vinogradova, Maia, Zhou, Wei, Liang, Jun, Wang, Xiaojing
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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파네소이드 X 수용체 효능제 및 이의 용도
LAI ANDILIY G, GOVEK STEVEN P, NAGASAWA JOHNNY Y, DOUGLAS KARENSA L, SMITH NICHOLAS D
Year of Publication 25.10.2019
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Year of Publication 25.10.2019
Patent
Abstract 4757: A novel class of selective estrogen receptors degraders regresses tumors in pre-clinical models of endocrine-resistant breast cancer
Joseph, James D., Darimont, Beatrice, Govek, Steven, Brigham, Dan, Qian, Jing, Sensintaffar, John, Shao, Gang, Aparicio, Anna, Kahraman, Mehmet, Lai, Andiliy, Lee, Kyoung-Jin, Lu, Nhin, Nagasawa, Johnny, Moon, Michael, Rix, Peter, Smith, Nick, Hager, Jeff
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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TETRACYCLIC AUTOTAXIN INHIBITORS
HUTCHINSON JOHN HOWARD, LONERGAN DAVID, ROWBOTTOM MARTIN, LAI ANDILIY GOKCHING
Year of Publication 26.07.2016
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Year of Publication 26.07.2016
Patent
Abstract A37: A novel class of selective estrogen receptor degraders display activity in pre-clinical models of ERα+ ovarian cancer
Joseph, James D., Darimont, Beatrice, Govek, Steven, Brigham, Dan, Aparicio, Anna, Kahraman, Mehmet, Lai, Andiliy, Lee, Kyoung-Jin, Lu, Nhin, Nagasawa, Johnny, Kaufman, Josh, Moon, Michael, Prudente, Rene, Qian, Jing, Sensintaffar, John, Shao, Gang, Rix, Peter, Smith, Nick, Hager, Jeff
Published in Clinical cancer research (01.10.2013)
Published in Clinical cancer research (01.10.2013)
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