Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor†

by England, Katherine S., Tumber, Anthony, Krojer, Tobias, Scozzafava, Giuseppe, Ng, Stanley S., Daniel, Michelle, Szykowska, Aleksandra, Che, KaHing, von Delft, Frank, Burgess-Brown, Nicola A., Kawamura, Akane, Schofield, Christopher J., Brennan, Paul E.
Published 2014

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

by Bavetsias, Vassilios, Lanigan, Rachel M., Ruda, Gian Filippo, Atrash, Butrus, McLaughlin, Mark G., Tumber, Anthony, Mok, N. Yi, Le Bihan, Yann-Vaï, Dempster, Sally, Boxall, Katherine J., Jeganathan, Fiona, Hatch, Stephanie B., Savitsky, Pavel, Velupillai, Srikannathasan, Krojer, Tobias, England, Katherine S., Sejberg, Jimmy, Thai, Ching, Donovan, Adam, Pal, Akos, Scozzafava, Giuseppe, Bennett, James M., Kawamura, Akane, Johansson, Catrine, Szykowska, Aleksandra, Gileadi, Carina, Burgess-Brown, Nicola A., von Delft, Frank, Oppermann, Udo, Walters, Zoe, Shipley, Janet, Raynaud, Florence I., Westaway, Susan M., Prinjha, Rab K., Fedorov, Oleg, Burke, Rosemary, Schofield, Christopher J., Westwood, Isaac M., Bountra, Chas, Müller, Susanne, van Montfort, Rob L. M., Brennan, Paul E., Blagg, Julian
Published 2016