A small molecule inhibitor of HER3: a proof-of-concept study
Colomba, Audrey, Fitzek, Martina, George, Roger, Weitsman, Gregory, Roberts, Selene, Zanetti-Domingues, Laura, Hirsch, Michael, Rolfe, Daniel J, Mehmood, Shahid, Madin, Andrew, Claus, Jeroen, Kjaer, Svend, Snijders, Ambrosius P, Ng, Tony, Martin-Fernandez, Marisa, Smith, David M, Parker, Peter J
Published in Biochemical journal (18.09.2020)
Published in Biochemical journal (18.09.2020)
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Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion
Kidd, Sarah L, Fowler, Elaine, Reinhardt, Till, Compton, Thomas, Mateu, Natalia, Newman, Hector, Bellini, Dom, Talon, Romain, McLoughlin, Joseph, Krojer, Tobias, Aimon, Anthony, Bradley, Anthony, Fairhead, Michael, Brear, Paul, Díaz-Sáez, Laura, McAuley, Katherine, Sore, Hannah F, Madin, Andrew, O'Donovan, Daniel H, Huber, Kilian V. M, Hyvönen, Marko, von Delft, Frank, Dowson, Christopher G, Spring, David R
Published in Chemical science (Cambridge) (21.10.2020)
Published in Chemical science (Cambridge) (21.10.2020)
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Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase
Read, Jon, Collie, Iain T., Nguyen-McCarty, Michelle, Lucaj, Christopher, Robinson, James, Conway, Leslie, Mukherjee, Jayanta, McCall, Eileen, Donohoe, Gerard, Flavell, Elizabeth, Peciak, Karolina, Warwicker, Juli, Dix, Carly, Van den Hoven, Bernard G., Madin, Andrew, Brown, Dean G., Moss, Stephen, Haggarty, Stephen J., Brandon, Nicholas J., Bürli, Roland W.
Published in Bioorganic & medicinal chemistry letters (01.08.2019)
Published in Bioorganic & medicinal chemistry letters (01.08.2019)
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Use of the Intramolecular Heck Reaction for Forming Congested Quaternary Carbon Stereocenters. Stereocontrolled Total Synthesis of (±)-Gelsemine
Madin, Andrew, O'Donnell, Christopher J, Oh, Taeboem, Old, David W, Overman, Larry E, Sharp, Matthew J
Published in Journal of the American Chemical Society (28.12.2005)
Published in Journal of the American Chemical Society (28.12.2005)
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Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition
Kennedy, Amanda J., Sundström, Linda, Geschwindner, Stefan, Poon, Eunice K. Y., Jiang, Yuhong, Chen, Rongfeng, Cooke, Rob, Johnstone, Shawn, Madin, Andrew, Lim, Junxian, Liu, Qingqi, Lohman, Rink-Jan, Nordqvist, Anneli, Fridén-Saxin, Maria, Yang, Wenzhen, Brown, Dean G., Fairlie, David P., Dekker, Niek
Published in Communications biology (17.12.2020)
Published in Communications biology (17.12.2020)
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Aza-Cope Rearrangement−Mannich Cyclizations for the Formation of Complex Tricyclic Amines: Stereocontrolled Total Synthesis of (±)-Gelsemine
Earley, William G, Jacobsen, Jon E, Madin, Andrew, Meier, G. Patrick, O'Donnell, Christopher J, Oh, Taeboem, Old, David W, Overman, Larry E, Sharp, Matthew J
Published in Journal of the American Chemical Society (28.12.2005)
Published in Journal of the American Chemical Society (28.12.2005)
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High Fidelity Suzuki–Miyaura Coupling for the Synthesis of DNA Encoded Libraries Enabled by Micelle Forming Surfactants
Hunter, James H, Prendergast, Lisa, Valente, Louis F, Madin, Andrew, Pairaudeau, Garry, Waring, Michael J
Published in Bioconjugate chemistry (15.01.2020)
Published in Bioconjugate chemistry (15.01.2020)
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Functional Group Tolerance of a Micellar on-DNA Suzuki–Miyaura Cross-Coupling Reaction for DNA-Encoded Library Design
Hunter, James H, Potowski, Marco, Stanway-Gordon, Harriet A, Madin, Andrew, Pairaudeau, Garry, Brunschweiger, Andreas, Waring, Michael J
Published in Journal of organic chemistry (17.12.2021)
Published in Journal of organic chemistry (17.12.2021)
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Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein–Ligand Interactions and High Selectivity
Collie, Gavin W., Clark, Matthew A., Keefe, Anthony D., Madin, Andrew, Read, Jon A., Rivers, Emma L., Zhang, Ying
Published in Journal of medicinal chemistry (25.01.2024)
Published in Journal of medicinal chemistry (25.01.2024)
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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs
Johannes, Jeffrey W., Balazs, Amber, Barratt, Derek, Bista, Michal, Chuba, Matthew D., Cosulich, Sabina, Critchlow, Susan E., Degorce, Sebastien L., Di Fruscia, Paolo, Edmondson, Scott D., Embrey, Kevin, Fawell, Stephen, Ghosh, Avipsa, Gill, Sonja J., Gunnarsson, Anders, Hande, Sudhir M., Heightman, Tom D., Hemsley, Paul, Illuzzi, Giuditta, Lane, Jordan, Larner, Carrie, Leo, Elisabetta, Liu, Lina, Madin, Andrew, Martin, Scott, McWilliams, Lisa, O'Connor, Mark J., Orme, Jonathan P., Pachl, Fiona, Packer, Martin J., Pei, Xiaohui, Pike, Andrew, Schimpl, Marianne, She, Hongyao, Staniszewska, Anna D., Talbot, Verity, Underwood, Elizabeth, Varnes, Jeffrey G., Xue, Lin, Yao, Tieguang, Zhang, Ke, Zhang, Andrew X., Zheng, Xiaolan
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries
Castan, Isaline F.S.F., Madin, Andrew, Pairaudeau, Garry, Waring, Michael J.
Published in Bioorganic & medicinal chemistry (01.06.2022)
Published in Bioorganic & medicinal chemistry (01.06.2022)
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Synthesis of Structurally Diverse N‐Substituted Quaternary‐Carbon‐Containing Small Molecules from α,α‐Disubstituted Propargyl Amino Esters
Mateu, Natalia, Kidd, Sarah L., Kalash, Leen, Sore, Hannah F., Madin, Andrew, Bender, Andreas, Spring, David R.
Published in Chemistry : a European journal (12.09.2018)
Published in Chemistry : a European journal (12.09.2018)
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Partially Saturated Bicyclic Heteroaromatics as an sp(3)-Enriched Fragment Collection
Twigg, David G., Kondo, Noriyasu, Mitchell, Sophie L., Galloway, Warren R. J. D., Sore, Hannah F., Madin, Andrew, Spring, David R.
Published in Angewandte Chemie International Edition (26.09.2016)
Published in Angewandte Chemie International Edition (26.09.2016)
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A small-molecule PI3Kα activator for cardioprotection and neuroregeneration
Gong, Grace Q., Bilanges, Benoit, Allsop, Ben, Masson, Glenn R., Roberton, Victoria, Askwith, Trevor, Oxenford, Sally, Madsen, Ralitsa R., Conduit, Sarah E., Bellini, Dom, Fitzek, Martina, Collier, Matt, Najam, Osman, He, Zhenhe, Wahab, Ben, McLaughlin, Stephen H., Chan, A. W. Edith, Feierberg, Isabella, Madin, Andrew, Morelli, Daniele, Bhamra, Amandeep, Vinciauskaite, Vanesa, Anderson, Karen E., Surinova, Silvia, Pinotsis, Nikos, Lopez-Guadamillas, Elena, Wilcox, Matthew, Hooper, Alice, Patel, Chandni, Whitehead, Maria A., Bunney, Tom D., Stephens, Len R., Hawkins, Phillip T., Katan, Matilda, Yellon, Derek M., Davidson, Sean M., Smith, David M., Phillips, James B., Angell, Richard, Williams, Roger L., Vanhaesebroeck, Bart
Published in Nature (London) (01.06.2023)
Published in Nature (London) (01.06.2023)
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Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries
Hunter, James H, Anderson, Matthew J, Castan, Isaline F. S. F, Graham, Jessica S, Salvini, Catherine L. A, Stanway-Gordon, Harriet A, Crawford, James J, Madin, Andrew, Pairaudeau, Garry, Waring, Michael J
Published in Chemical science (Cambridge) (14.07.2021)
Published in Chemical science (Cambridge) (14.07.2021)
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AiZynth impact on medicinal chemistry practice at AstraZeneca
Shields, Jason D, Howells, Rachel, Lamont, Gillian, Leilei, Yin, Madin, Andrew, Reimann, Christopher E, Rezaei, Hadi, Reuillon, Tristan, Smith, Bryony, Thomson, Clare, Zheng, Yuting, Ziegler, Robert E
Published in MedChemComm (24.04.2024)
Published in MedChemComm (24.04.2024)
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Discovery of a selective c-MET inhibitor with a novel binding mode
Collie, Gavin W., Barlind, Louise, Bazzaz, Sana, Börjesson, Ulf, Dale, Ian L., Disch, Jeremy S., Habeshian, Sevan, Jetson, Rachael, Khurana, Puneet, Madin, Andrew, Michaelides, Iacovos N., Peng, Ling, Snijder, Arjan, Stubbs, Christopher J.
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
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Abstract 296: Structure-based and property-based drug design of AZD5305, a highly selective PARP1 inhibitor and trapper
Hande, Sudhir, Balazs, Amber, Degorce, Sébastien L., Embrey, Kevin, Ghosh, Avipsa, Gill, Sonja J., Gunnarsson, Anders, Illuzzi, Giuditta, Lane, Jordan, Larner, Carrie, Leo, Elisabetta, Madin, Andrew, McWilliams, Lisa, O'Connor, Mark J., Orme, Jonathan, Pachl, Fiona, Packer, Martin, Pike, Andy, Rawlins, Philip, Schimpl, Marianne, Staniszewska, Anna D., Zhang, Andrew, Zheng, Xiaolan, Johannes, Jeffrey W.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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