Structure-Based Optimization of a Series of Covalent, Cell Active Bfl‑1 Inhibitors
Lucas, Simon C. C., Blackwell, J. Henry, Börjesson, Ulf, Hargreaves, David, Milbradt, Alexander G., Bostock, Mark J., Ahmed, Samiyah, Beaumont, Kevin, Cheung, Tony, Demanze, Sylvain, Gohlke, Andrea, Guerot, Carine, Haider, Afreen, Kantae, Vasudev, Kauffman, Gregory W., Kinzel, Olaf, Kupcova, Lea, Lainchbury, Michael D., Lamb, Michelle L., Leon, Leonardo, Palisse, Adeline, Sacchetto, Claudia, Storer, R. Ian, Su, Nancy, Thomson, Clare, Vales, John, Chen, Yunhua, Hu, Xiaolong
Published in Journal of medicinal chemistry (26.09.2024)
Published in Journal of medicinal chemistry (26.09.2024)
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Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation
Hanan, Emily J, Eigenbrot, Charles, Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Dotson, Jennafer, Heald, Robert A, Jackson, Philip S, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Tam, Christine, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yin, Jianping, Yu, Christine, Zilberleyb, Inna, Heffron, Timothy P
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Journal Article
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor
Chan, Bryan K, Hanan, Emily J, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dela Vega, Trisha, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard L, Heald, Robert A, Jackson, Philip S, Knight, Jamie D, La, Hank, Lainchbury, Michael D, Malek, Shiva, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen M, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Siew Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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Journal Article
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study
Heald, Robert, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Bryan, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dominguez-Fernandez, Belen, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Jackson, Philip, Knight, Jamie, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam, Merchant, Mark, Mortara, Kyle, Purkey, Hans, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (25.11.2015)
Published in Journal of medicinal chemistry (25.11.2015)
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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1
Tellis, John C, Wei, BinQing, Siu, Michael, An, Le, Chan, Grace Kayan, Chen, Yong, Du, Xiangnan, Gazzard, Lewis, Hu, Baihua, Kiefer, James, Kakiuchi-Kiyota, Satoko, Lainchbury, Michael, Linehan, Jonathan L, Luo, Xifeng, Malhotra, Sushant, Mendonca, Rohan, Pang, Jodie, Ran, Yinqing, Sethuraman, Vijay, Seward, Eileen, Sneeringer, Chris, Su, Dian, Wang, Weiru, Wu, Ping, Moffat, John G, Heffron, Timothy P, Choo, Edna F, Chan, Bryan K
Published in ACS medicinal chemistry letters (12.09.2024)
Published in ACS medicinal chemistry letters (12.09.2024)
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Journal Article
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma
Walton, Mike I., Eve, Paul D., Hayes, Angela, Henley, Alan T., Valenti, Melanie R., De Haven Brandon, Alexis K., Box, Gary, Boxall, Kathy J., Tall, Matthew, Swales, Karen, Matthews, Thomas P., McHardy, Tatiana, Lainchbury, Michael, Osborne, James, Hunter, Jill E., Perkins, Neil D., Aherne, G. Wynne, Reader, John C., Raynaud, Florence I., Eccles, Suzanne A., Collins, Ian, Garrett, Michelle D.
Published in Oncotarget (19.01.2016)
Published in Oncotarget (19.01.2016)
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Fragment screening at AstraZeneca: developing the next generation biophysics fragment set
Lucas, Simon C. C, Börjesson, Ulf, Bostock, Mark J, Cuff, John, Edfeldt, Fredrik, Embrey, Kevin J, Eriksson, Per-Olof, Gohlke, Andrea, Gunnarson, Anders, Lainchbury, Michael, Milbradt, Alexander G, Moore, Rachel, Rawlins, Philip B, Sinclair, Ian, Stubbs, Christopher, Storer, R. Ian
Published in MedChemComm (21.09.2022)
Published in MedChemComm (21.09.2022)
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5-[[4-[[-2-]]-5--2-]]-2- 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-TRIFLUOROMETHYL-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
LAINCHBURY MICHAEL, MATTHEWS THOMAS PETER, FARIA DA FONSECA MCHARDY TATIANA, OSBORNE JAMES, WALTON MICHAEL IAN, GARRETT MICHELLE DAWN, COLLINS IAN
Year of Publication 22.02.2024
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Year of Publication 22.02.2024
Patent
CCT244747 Is a Novel Potent and Selective CHK1 Inhibitor with Oral Efficacy Alone and in Combination with Genotoxic Anticancer Drugs
WALTON, Mike I, EVE, Paul D, MATTHEWS, Thomas P, JAMIN, Yann, ROBINSON, Simon P, WYNNEAHERNE, G, READER, John C, CHESLER, Louis, RAYNAUD, Florence I, ECCLES, Suzanne A, COLLINS, Ian, GARRETT, Michelle D, HAYES, Angela, VALENTI, Melanie R, DE HAVEN BRANDON, Alexis K, BOX, Gary, HALLSWORTH, Albert, SMITH, Elizabeth L, BOXALL, Kathy J, LAINCHBURY, Michael
Published in Clinical cancer research (15.10.2012)
Published in Clinical cancer research (15.10.2012)
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Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)
Chan, Bryan K, Seward, Eileen, Lainchbury, Michael, Brewer, Thomas F, An, Le, Blench, Toby, Cartwright, Matthew W, Chan, Grace Ka Yan, Choo, Edna F, Drummond, Jason, Elliott, Richard L, Gancia, Emanuela, Gazzard, Lewis, Hu, Baihua, Jones, Graham E, Luo, Xifeng, Madin, Andrew, Malhotra, Sushant, Moffat, John G, Pang, Jodie, Salphati, Laurent, Sneeringer, Christopher J, Stivala, Craig E, Wei, Binqing, Wang, Weiru, Wu, Ping, Heffron, Timothy P
Published in ACS medicinal chemistry letters (13.01.2022)
Published in ACS medicinal chemistry letters (13.01.2022)
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Journal Article
5-[[4-[[-2-]]-5--2-]]-2- 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-TRIFLUOROMETHYL-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
LAINCHBURY MICHAEL, MATTHEWS THOMAS PETER, FARIA DA FONSECA MCHARDY TATIANA, OSBORNE JAMES, WALTON MICHAEL IAN, GARRETT MICHELLE DAWN, COLLINS IAN
Year of Publication 11.11.2022
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Year of Publication 11.11.2022
Patent
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)‑5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737)
Osborne, James D, Matthews, Thomas P, McHardy, Tatiana, Proisy, Nicolas, Cheung, Kwai-Ming J, Lainchbury, Michael, Brown, Nathan, Walton, Michael I, Eve, Paul D, Boxall, Katherine J, Hayes, Angela, Henley, Alan T, Valenti, Melanie R, De Haven Brandon, Alexis K, Box, Gary, Jamin, Yann, Robinson, Simon P, Westwood, Isaac M, van Montfort, Rob L. M, Leonard, Philip M, Lamers, Marieke B. A. C, Reader, John C, Aherne, G. Wynne, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian
Published in Journal of medicinal chemistry (09.06.2016)
Published in Journal of medicinal chemistry (09.06.2016)
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Journal Article
5-[[4-[[-2-]]-5--2-]]-2- 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-TRIFLUOROMETHYL-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
LAINCHBURY MICHAEL, MATTHEWS THOMAS PETER, FARIA DA FONSECA MCHARDY TATIANA, OSBORNE JAMES, WALTON MICHAEL IAN, GARRETT MICHELLE DAWN, COLLINS IAN
Year of Publication 24.12.2021
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Year of Publication 24.12.2021
Patent
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR
Bryan, Marian C, Burdick, Daniel J, Chan, Bryan K, Chen, Yuan, Clausen, Saundra, Dotson, Jennafer, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Heald, Robert, Jackson, Philip, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam E, Purkey, Hans E, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Wang, Shumei, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in ACS medicinal chemistry letters (14.01.2016)
Published in ACS medicinal chemistry letters (14.01.2016)
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Journal Article
5-[[4-[[-2-]]-5--2-]]-2- 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-TRIFLUOROMETHYL-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
LAINCHBURY MICHAEL, MATTHEWS THOMAS PETER, FARIA DA FONSECA MCHARDY TATIANA, OSBORNE JAMES, WALTON MICHAEL IAN, GARRETT MICHELLE DAWN, COLLINS IAN
Year of Publication 30.04.2021
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Year of Publication 30.04.2021
Patent
Discovery of 3‑Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors
Lainchbury, Michael, Matthews, Thomas P, McHardy, Tatiana, Boxall, Kathy J, Walton, Michael I, Eve, Paul D, Hayes, Angela, Valenti, Melanie R, de Haven Brandon, Alexis K, Box, Gary, Aherne, G. Wynne, Reader, John C, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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Journal Article
Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study
Heald, Robert, Bowman, Krista K, Bryan, Marian C, Burdick, Daniel, Chan, Bryan, Chan, Emily, Chen, Yuan, Clausen, Saundra, Dominguez-Fernandez, Belen, Eigenbrot, Charles, Elliott, Richard, Hanan, Emily J, Jackson, Philip, Knight, Jamie, La, Hank, Lainchbury, Michael, Malek, Shiva, Mann, Sam, Merchant, Mark, Mortara, Kyle, Purkey, Hans, Schaefer, Gabriele, Schmidt, Stephen, Seward, Eileen, Sideris, Steve, Shao, Lily, Wang, Shumei, Yeap, Kuen, Yen, Ivana, Yu, Christine, Heffron, Timothy P
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
5-[[4-[[-2-]]-5--2-]]-2- 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-TRIFLUOROMETHYL-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF
LAINCHBURY MICHAEL, MATTHEWS THOMAS PETER, FARIA DA FONSECA MCHARDY TATIANA, OSBORNE JAMES, WALTON MICHAEL IAN, GARRETT MICHELLE DAWN, COLLINS IAN
Year of Publication 14.04.2020
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Year of Publication 14.04.2020
Patent