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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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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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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SHP2 25- 3- 256-3 3- 25-DISUBSTITUTED 3-METHYL PYRAZINES AND 256- TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS
BUCKL ANDREAS, KISS GERT, WON WALTER, KOLTUN ELENA S, SEMKO CHRISTOPHER, JOGALEKAR ASHUTOSH, AAY NAING, MELLEM KEVIN, GILL ADRIAN
Year of Publication 13.11.2023
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Year of Publication 13.11.2023
Patent
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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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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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
RAS 억제제
BUCKL ANDREAS, BURNETT G. LESLIE, WHALEN DANIEL M, KOLTUN ELENA S, GILL ADRIAN L, CREGG JAMES, AAY NAING, PITZEN JENNIFER, LIU YANG, KNOX JOHN E, AGGEN JAMES
Year of Publication 04.08.2022
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Year of Publication 04.08.2022
Patent
암의 치료에서 RAS 억제제로서 인돌 유도체
BUCKL ANDREAS, BURNETT G. LESLIE, RICE MEGHAN A, KOLTUN ELENA S, WILDES DAVID E, GILL ADRIAN L, LEE BIANCA JENNIFER, SINGH MALLIKA, CREGG JAMES, AAY NAING, LIU YANG, KNOX JOHN E
Year of Publication 16.05.2023
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Year of Publication 16.05.2023
Patent
이환식 헤테로사이클릴 화합물 및 이의 용도
BUCKL ANDREAS, TAMBO ONG ARLYN A, CREGG JAMES JOSEPH, KOLTUN ELENA S, THOMPSON SEVERIN, GLIEDT MICAH J, AAY NAING, GILL ADRIAN LIAM
Year of Publication 03.12.2021
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Year of Publication 03.12.2021
Patent
이환식 헤테로아릴 화합물 및 이의 용도
BUCKL ANDREAS, TAMBO ONG ARLYN A, CREGG JAMES JOSEPH, KOLTUN ELENA S, THOMPSON SEVERIN, GLIEDT MICAH J, AAY NAING, GILL ADRIAN LIAM
Year of Publication 03.12.2021
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Year of Publication 03.12.2021
Patent
이환식 헤테로아릴 화합물 및 이의 용도
BUCKL ANDREAS, TAMBO ONG ARLYN A, BURNETT G. LESLIE, THOMPSON SEVERIN, AAY NAING, LIU YANG, GILL ADRIAN LIAM, EDWARDS ANNE V, KOLTUN ELENA S, CREGG JAMES JOSEPH, GLIEDT MICAH J, THOMAS WILLIAM D, KNOX JOHN E
Year of Publication 18.07.2022
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Year of Publication 18.07.2022
Patent
알로스테릭 SHP2 억제제로서의 피리딘 화합물
BUCKL ANDREAS, KISS GERT, KOLTUN ELENA S, SEMKO CHRISTOPHER, AAY NAING, MELLEM KEVIN, GILL ADRIAN
Year of Publication 30.09.2019
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Year of Publication 30.09.2019
Patent
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
알로스테릭 SHP2 억제제로서의 피리딘, 피라진 및 트리아진 화합물
BUCKL ANDREAS, TZITZILONIS CHRISTOS, WON WALTER, KOLTUN ELENA S, CREGG JAMES JOSEPH, LI JIE JACK, AAY NAING, JOGALEKAR ASHUTOSH, MELLEM KEVIN, GILL ADRIAN LIAM
Year of Publication 17.06.2020
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Year of Publication 17.06.2020
Patent
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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다른자리 입체성 SHP2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
BUCKL ANDREAS, KISS GERT, WON WALTER, KOLTUN ELENA S, SEMKO CHRISTOPHER, JOGALEKAR ASHUTOSH, AAY NAING, MELLEM KEVIN, GILL ADRIAN
Year of Publication 13.03.2019
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Year of Publication 13.03.2019
Patent
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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