Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)
Rice, Kenneth D, Aay, Naing, Anand, Neel K, Blazey, Charles M, Bowles, Owen J, Bussenius, Joerg, Costanzo, Simona, Curtis, Jeffry K, Defina, Steven C, Dubenko, Larisa, Engst, Stefan, Joshi, Anagha A, Kennedy, Abigail R, Kim, Angie I, Koltun, Elena S, Lougheed, Julie C, Manalo, Jean-Claire L, Martini, Jean-Francois, Nuss, John M, Peto, Csaba J, Tsang, Tsze H, Yu, Peiwen, Johnston, Stuart
Published in ACS medicinal chemistry letters (10.05.2012)
Published in ACS medicinal chemistry letters (10.05.2012)
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Journal Article
Discovery of XL413, a potent and selective CDC7 inhibitor
Koltun, Elena S., Tsuhako, Amy Lew, Brown, David S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Ferguson, Kim, Franzini, Maurizio, Galan, Adam, Holst, Charles R., Huang, Ping, Kane, Brian, Kim, Moon H., Li, Jia, Markby, David, Mohan, Manisha, Noson, Kevin, Plonowski, Arthur, Richards, Steven J., Robertson, Scott, Shaw, Kenneth, Stott, Gordon, Stout, Thomas J., Young, Jenny, Yu, Peiwen, Zaharia, Cristiana A., Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Xu, Wei, Kearney, Patrick C.
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Discovery of XL888: A novel tropane-derived small molecule inhibitor of HSP90
Bussenius, Joerg, Blazey, Charles M., Aay, Naing, Anand, Neel K., Arcalas, Arlyn, Baik, TaeGon, Bowles, Owen J., Buhr, Chris A., Costanzo, Simona, Curtis, Jeffrey K., DeFina, Steven C., Dubenko, Larisa, Heuer, Timothy S., Huang, Ping, Jaeger, Christopher, Joshi, Anagha, Kennedy, Abigail R., Kim, Angie I., Lara, Katherine, Lee, Jae, Li, Jonathan, Lougheed, Julie C., Ma, Sunghoon, Malek, Shiva, Manalo, Jean-Claire L., Martini, Jean-Francois, McGrath, Garth, Nicoll, Monique, Nuss, John M., Pack, Michael, Peto, Csaba J., Tsang, Tsze H., Wang, Longcheng, Womble, Scott W., Yakes, Michael, Zhang, Wentao, Rice, Kenneth D.
Published in Bioorganic & medicinal chemistry letters (01.09.2012)
Published in Bioorganic & medicinal chemistry letters (01.09.2012)
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Journal Article
Discovery of a new class of glucosylceramide synthase inhibitors
Koltun, Elena, Richards, Steven, Chan, Vicky, Nachtigall, Jason, Du, Hongwang, Noson, Kevin, Galan, Adam, Aay, Naing, Hanel, Art, Harrison, Amanda, Zhang, Jeff, Won, Kwang-Ai, Tam, Danny, Qian, Fawn, Wang, Tao, Finn, Patricia, Ogilvie, Kathleen, Rosen, Jon, Mohan, Raju, Larson, Christopher, Lamb, Peter, Nuss, John, Kearney, Patrick
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
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Journal Article
Abstract 1273: Discovery of a potent, selective, and orally bioavailable SOS1 inhibitor, RMC-023, an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction
Buckl, Andreas, Quintana, Elsa, Lee, Grace J., Shifrin, Nataliya, Zhong, Mengqi, Garrenton, Lindsay S., Montgomery, David C., Stahlhut, Carlos, Zhao, Frances, Whalen, Dan M., Thompson, Severin K., Tambo-ong, Arlyn, Gliedt, Micah, Knox, John E., Cregg, James J., Aay, Naing, Choi, Jong, Nguyen, Bao, Tripathi, Atti, Zhao, Ruiping, Saldajeno-Concar, Mae, Marquez, Abby, Hsieh, Daphne, McDowell, Laura L., Koltun, Elena S., Bermingham, Alun, Wildes, David, Singh, Mallika, Wang, Zhengping, Hansen, Richard, Smith, Jan A., Gill, Adrian L.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Journal Article
Discovery of a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR)
Takeuchi, Craig S, Kim, Byung Gyu, Blazey, Charles M, Ma, Sunghoon, Johnson, Henry W. B, Anand, Neel K, Arcalas, Arlyn, Baik, Tae Gon, Buhr, Chris A, Cannoy, Jonah, Epshteyn, Sergey, Joshi, Anagha, Lara, Katherine, Lee, Matthew S, Wang, Longcheng, Leahy, James W, Nuss, John M, Aay, Naing, Aoyama, Ron, Foster, Paul, Lee, Jae, Lehoux, Isabelle, Munagala, Narsimha, Plonowski, Arthur, Rajan, Sharmila, Woolfrey, John, Yamaguchi, Kyoko, Lamb, Peter, Miller, Nicole
Published in Journal of medicinal chemistry (28.03.2013)
Published in Journal of medicinal chemistry (28.03.2013)
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Journal Article
Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity
Koltun, Elena S., Aay, Naing, Buckl, Andreas, Jogalekar, Ashutosh S., Kiss, Gert, Marquez, Abby, Mellem, Kevin T., Mordec, Kasia, Saldajeno-Concar, Mae, Semko, Chris M., Tibrewal, Nidhi, Tzitzilonis, Christos, Won, Walter, Smith, Jacqueline A., Wilson, Susan E., Nichols, Robert J., Wang, Zhengping, Wilds, David, Singh, Mallika, Gill, Adrian L.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Abstract 4877: Allosteric inhibition of SHP2 variants containing cancer-associated activating mutations
Wildes, David, Aay, Naing, Buckl, Andreas, Hsieh, Daphne, Jogalekar, Ashutosh S., Kiss, Gert, Koltun, Elena S., Marquez, Abby, Mellem, Kevin T., Romero, Jason, Saldajeno-Concar, Mae, Schulze, Christopher J., Semko, Chris M., Won, Walter, Nichols, Robert J., Stahlhut, Carlos, Tzitzilonis, Christos, Gill, Adrian L., Smith, Jacqueline A.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
The design, synthesis, and biological evaluation of PIM kinase inhibitors
Tsuhako, Amy Lew, Brown, David S., Koltun, Elena S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Franzini, Maurizio, Galan, Adam, Huang, Ping, Johnston, Stuart, Kane, Brian, Kim, Moon H., Douglas Laird, A., Lin, Rui, Mock, Lillian, Ngan, Iris, Pack, Michael, Stott, Gordon, Stout, Thomas J., Yu, Peiwen, Zaharia, Cristiana, Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Kearney, Patrick C., Xu, Wei
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Discovery and Characterization of an Inhibitor of Glucosylceramide Synthase
Richards, Steven, Larson, Christopher J, Koltun, Elena S, Hanel, Art, Chan, Vicky, Nachtigall, Jason, Harrison, Amanda, Aay, Naing, Du, Hongwang, Arcalas, Arlyn, Galan, Adam, Zhang, Jeff, Zhang, Wentao, Won, Kwang-Ai, Tam, Danny, Qian, Fawn, Wang, Tao, Finn, Patricia, Ogilvie, Kathy, Rosen, Jon, Aoyama, Ron, Plonowski, Artur, Cancilla, Belinda, Bentzien, Frauke, Yakes, Michael, Mohan, Raju, Lamb, Peter, Nuss, John, Kearney, Patrick
Published in Journal of medicinal chemistry (10.05.2012)
Published in Journal of medicinal chemistry (10.05.2012)
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Journal Article
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors
Forsyth, Timothy, Kearney, Patrick C., Kim, Byung Gyu, Johnson, Henry W.B., Aay, Naing, Arcalas, Arlyn, Brown, David S., Chan, Vicky, Chen, Jeff, Du, Hongwang, Epshteyn, Sergey, Galan, Adam A., Huynh, Tai P., Ibrahim, Mohamed A., Kane, Brian, Koltun, Elena S., Mann, Grace, Meyr, Lisa E., Lee, Matthew S., Lewis, Gary L., Noguchi, Robin T., Pack, Michael, Ridgway, Brian H., Shi, Xian, Takeuchi, Craig S., Zu, Peiwen, Leahy, James W., Nuss, John M., Aoyama, Ron, Engst, Stefan, Gendreau, Steven B., Kassees, Robert, Li, Jia, Lin, Shwu-Hwa, Martini, Jean-Francois, Stout, Thomas, Tong, Philip, Woolfrey, John, Zhang, Wentao, Yu, Peiwen
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
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Journal Article
Erratum to “Discovery of XL413, a potent and selective CDC7 inhibitor” [Bioorg. Med. Chem. Lett. 22 (2012) 3727–3731]
Koltun, Elena S., Tsuhako, Amy Lew, Brown, David S., Aay, Naing, Arcalas, Arlyn, Chan, Vicky, Du, Hongwang, Engst, Stefan, Ferguson, Kim, Franzini, Maurizio, Galan, Adam, Holst, Charles R., Huang, Ping, Kane, Brian, Kim, Moon H., Li, Jia, Markby, David, Mohan, Manisha, Noson, Kevin, Plonowski, Arthur, Richards, Steven J., Robertson, Scott, Shaw, Kenneth, Stott, Gordon, Stout, Thomas J., Young, Jenny, Yu, Peiwen, Zaharia, Cristiana A., Zhang, Wentao, Zhou, Peiwen, Nuss, John M., Xu, Wei, Kearney, Patrick C.
Published in Bioorganic & medicinal chemistry letters (01.08.2012)
Published in Bioorganic & medicinal chemistry letters (01.08.2012)
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Journal Article
PYRIDINE COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
KISS, Gert, GILL, Adrian, AAY, Naing, MELLEM, Kevin, SEMKO, Christopher, BUCKL, Andreas, KOLTUN, Elena S
Year of Publication 21.03.2024
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Year of Publication 21.03.2024
Patent
PYRIDINE COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
KISS, Gert, GILL, Adrian, AAY, Naing, MELLEM, Kevin, SEMKO, Christopher, BUCKL, Andreas, KOLTUN, Elena S
Year of Publication 11.10.2023
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Year of Publication 11.10.2023
Patent
PYRIDINE COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
KISS, Gert, GILL, Adrian, AAY, Naing, MELLEM, Kevin, SEMKO, Christopher, BUCKL, Andreas, KOLTUN, Elena S
Year of Publication 23.08.2023
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Year of Publication 23.08.2023
Patent
Pyridine compounds as allosteric SHP2 inhibitors
Koltun, Elena S, Gill, Adrian, Mellem, Kevin, Semko, Christopher, Kiss, Gert, Aay, Naing, Buckl, Andreas
Year of Publication 13.06.2023
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Year of Publication 13.06.2023
Patent