A novel tankyrase inhibitor, MSC2504877, enhances the effects of clinical CDK4/6 inhibitors
Menon, Malini, Elliott, Richard, Bowers, Leandra, Balan, Nicolae, Rafiq, Rumana, Costa-Cabral, Sara, Munkonge, Felix, Trinidade, Ines, Porter, Roderick, Campbell, Andrew D, Johnson, Emma R, Esdar, Christina, Buchstaller, Hans-Peter, Leuthner, Birgitta, Rohdich, Felix, Schneider, Richard, Sansom, Owen, Wienke, Dirk, Ashworth, Alan, Lord, Christopher J
Published in Scientific reports (17.01.2019)
Published in Scientific reports (17.01.2019)
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3D imaging of colorectal cancer organoids identifies responses to Tankyrase inhibitors
Badder, Luned M, Hollins, Andrew J, Herpers, Bram, Yan, Kuan, Ewan, Kenneth B, Thomas, Mairian, Shone, Jennifer R, Badder, Delyth A, Naven, Marc, Ashelford, Kevin E, Hargest, Rachel, Clarke, Alan R, Esdar, Christina, Buchstaller, Hans-Peter, Treherne, J. Mark, Boj, Sylvia, Ramezanpour, Bahar, Wienke, Dirk, Price, Leo S, Shaw, Paul H, Dale, Trevor C
Published in PloS one (18.08.2020)
Published in PloS one (18.08.2020)
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A Novel Strategy for ADME Screening of Prodrugs: Combined Use of Serum and Hepatocytes to Integrate Bioactivation and Clearance, and Predict Exposure to Both Active and Prodrug to the Systemic Circulation
Hoppe, Edmund, Hewitt, Nicola J., Buchstaller, Hans-Peter, Eggenweiler, Hans-Michael, Sirrenberg, Christian, Zimmermann, Astrid, März, Joachim, Schwartz, Harry, Saal, Christoph, Meyring, Michael, Hecht, Stefan
Published in Journal of pharmaceutical sciences (01.05.2014)
Published in Journal of pharmaceutical sciences (01.05.2014)
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Journal Article
AIDDISON: Empowering Drug Discovery with AI/ML and CADD Tools in a Secure, Web-Based SaaS Platform
Rusinko, Andrew, Rezaei, Mohammad, Friedrich, Lukas, Buchstaller, Hans-Peter, Kuhn, Daniel, Ghogare, Ashwini
Published in Journal of chemical information and modeling (08.01.2024)
Published in Journal of chemical information and modeling (08.01.2024)
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Estimation of Drug-Target Residence Times by τ‑Random Acceleration Molecular Dynamics Simulations
Kokh, Daria B, Amaral, Marta, Bomke, Joerg, Grädler, Ulrich, Musil, Djordje, Buchstaller, Hans-Peter, Dreyer, Matthias K, Frech, Matthias, Lowinski, Maryse, Vallee, Francois, Bianciotto, Marc, Rak, Alexey, Wade, Rebecca C
Published in Journal of chemical theory and computation (10.07.2018)
Published in Journal of chemical theory and computation (10.07.2018)
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Large-Scale Assessment of Binding Free Energy Calculations in Active Drug Discovery Projects
Schindler, Christina E. M, Baumann, Hannah, Blum, Andreas, Böse, Dietrich, Buchstaller, Hans-Peter, Burgdorf, Lars, Cappel, Daniel, Chekler, Eugene, Czodrowski, Paul, Dorsch, Dieter, Eguida, Merveille K. I, Follows, Bruce, Fuchß, Thomas, Grädler, Ulrich, Gunera, Jakub, Johnson, Theresa, Jorand Lebrun, Catherine, Karra, Srinivasa, Klein, Markus, Knehans, Tim, Koetzner, Lisa, Krier, Mireille, Leiendecker, Matthias, Leuthner, Birgitta, Li, Liwei, Mochalkin, Igor, Musil, Djordje, Neagu, Constantin, Rippmann, Friedrich, Schiemann, Kai, Schulz, Robert, Steinbrecher, Thomas, Tanzer, Eva-Maria, Unzue Lopez, Andrea, Viacava Follis, Ariele, Wegener, Ansgar, Kuhn, Daniel
Published in Journal of chemical information and modeling (23.11.2020)
Published in Journal of chemical information and modeling (23.11.2020)
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Journal Article
Discovery and Optimization of 2‑Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity
Buchstaller, Hans-Peter, Anlauf, Uwe, Dorsch, Dieter, Kuhn, Daniel, Lehmann, Martin, Leuthner, Birgitta, Musil, Djordje, Radtki, Daniela, Ritzert, Claudio, Rohdich, Felix, Schneider, Richard, Esdar, Christina
Published in Journal of medicinal chemistry (12.09.2019)
Published in Journal of medicinal chemistry (12.09.2019)
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Journal Article
Identification of M4205A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors
Blum, Andreas, Dorsch, Dieter, Linde, Nina, Brandstetter, Susanne, Buchstaller, Hans-Peter, Busch, Michael, Glaser, Nina, Grädler, Ulrich, Ruff, Aaron, Petersson, Carl, Schieferstein, Hanno, Sherbetjian, Eva, Esdar, Christina
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
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Synthesis of Thieno[2,3-b]Pyridinones Acting as Cytoprotectants and as Inhibitors of [3H]Glycine Binding to the N-Methyl-d-aspartate (NMDA) Receptor
Buchstaller, Hans-Peter, Siebert, Carsten D, Steinmetz, Ralf, Frank, Ina, Berger, Michael L, Gottschlich, Rudolf, Leibrock, Joachim, Krug, Michael, Steinhilber, Dieter, Noe, Christian R
Published in Journal of medicinal chemistry (09.02.2006)
Published in Journal of medicinal chemistry (09.02.2006)
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Ligand Desolvation Steers On-Rate and Impacts Drug Residence Time of Heat Shock Protein 90 (Hsp90) Inhibitors
Schuetz, Doris A, Richter, Lars, Amaral, Marta, Grandits, Melanie, Grädler, Ulrich, Musil, Djordje, Buchstaller, Hans-Peter, Eggenweiler, Hans-Michael, Frech, Matthias, Ecker, Gerhard F
Published in Journal of medicinal chemistry (24.05.2018)
Published in Journal of medicinal chemistry (24.05.2018)
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Journal Article
Discovery of Cycloalkyl[c]thiophenes as Novel Scaffolds for Hypoxia-Inducible Factor-2α Inhibitors
Buchstaller, Hans-Peter, Sala-Hojman, Ada, Leiendecker, Matthias, Albers, Joachim, Anlauf, Uwe, Berges, Nina, Dong, Liming, Fuchß, Thomas, Germann, Martina, Knehans, Tim, Krier, Mireille, Lecomte, Marc, Müller, Daniel, Müller, Sandra R., Leuthner, Birgitta, Lindemann, Ralph, Musil, Djordje, Nowak, Mateusz, Reither, Vivian, Rettig, Corinna, Schindler, Christina E. M., Pakulska, Urszula, Spuck, Dieter, Wegener, Ansgar, Zarębski, Adrian
Published in Journal of medicinal chemistry (13.07.2023)
Published in Journal of medicinal chemistry (13.07.2023)
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Journal Article
Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models
Buchstaller, Hans-Peter, Anlauf, Uwe, Dorsch, Dieter, Kögler, Sarah, Kuhn, Daniel, Lehmann, Martin, Leuthner, Birgitta, Lodholz, Sara, Musil, Djordje, Radtki, Daniela, Rettig, Corinna, Ritzert, Claudio, Rohdich, Felix, Schneider, Richard, Wegener, Ansgar, Weigt, Stefan, Wilkinson, Kai, Esdar, Christina
Published in Journal of medicinal chemistry (22.07.2021)
Published in Journal of medicinal chemistry (22.07.2021)
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Journal Article
Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates
Heinrich, Timo, Buchstaller, Hans-Peter, Cezanne, Bertram, Rohdich, Felix, Bomke, Jörg, Friese-Hamim, Manja, Krier, Mireille, Knöchel, Thorsten, Musil, Djordje, Leuthner, Birgitta, Zenke, Frank
Published in Bioorganic & medicinal chemistry letters (01.02.2017)
Published in Bioorganic & medicinal chemistry letters (01.02.2017)
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Journal Article
The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5
SCHIEMANN, Kai, FINSINGER, Dirk, ZENKE, Frank, AMENDT, Christiane, KNÖCHEL, Thorsten, BRUGE, David, BUCHSTALLER, Hans-Peter, EMDE, Ulrich, STÄHLE, Wolfgang, ANZALI, Soheila
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Discovery of novel 7-azaindoles as PDK1 inhibitors
Wucherer-Plietker, Margarita, Merkul, Eugen, Müller, Thomas J.J., Esdar, Christina, Knöchel, Thorsten, Heinrich, Timo, Buchstaller, Hans-Peter, Greiner, Hartmut, Dorsch, Dieter, Finsinger, Dirk, Calderini, Michel, Bruge, David, Grädler, Ulrich
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
Published in Bioorganic & medicinal chemistry letters (01.07.2016)
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Journal Article
Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors
Buchstaller, Hans-Peter, Burgdorf, Lars, Finsinger, Dirk, Stieber, Frank, Sirrenberg, Christian, Amendt, Christiane, Grell, Matthias, Zenke, Frank, Krier, Mireille
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
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Journal Article
Fragment-based discovery of hydroxy-indazole-carboxamides as novel small molecule inhibitors of Hsp90
Buchstaller, Hans-Peter, Eggenweiler, Hans-Michael, Sirrenberg, Christian, Grädler, Ulrich, Musil, Djordje, Hoppe, Edmund, Zimmermann, Astrid, Schwartz, Harry, März, Joachim, Bomke, Jörg, Wegener, Ansgar, Wolf, Michael
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
Published in Bioorganic & medicinal chemistry letters (01.07.2012)
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