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Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies.
J Med Chem. 2019 Feb 28;62(4):2154-2171. doi: 10.1021/acs.jmedchem.8b01872. Epub 2019 Feb 11.
J Med Chem. 2019.
PMID: 30689376
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Bertrand SM, Ancellin N, Beaufils B, Bingham RP, Borthwick JA, Boullay AB, Boursier E, Carter PS, Chung CW, Churcher I, Dodic N, Fouchet MH, Fournier C, Francis PL, Gummer LA, Herry K, Hobbs A, Hobbs CI, Homes P, Jamieson C, Nicodeme E, Pickett SD, Reid IH, Simpson GL, Sloan LA, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Valko K, Washio Y, Young RJ.
Bertrand SM, et al.
J Med Chem. 2015 Sep 24;58(18):7140-63. doi: 10.1021/acs.jmedchem.5b00313. Epub 2015 Jul 2.
J Med Chem. 2015.
PMID: 26090771
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Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Borthwick JA, Ancellin N, Bertrand SM, Bingham RP, Carter PS, Chung CW, Churcher I, Dodic N, Fournier C, Francis PL, Hobbs A, Jamieson C, Pickett SD, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Young RJ.
Borthwick JA, et al.
J Med Chem. 2016 Mar 24;59(6):2452-67. doi: 10.1021/acs.jmedchem.5b01607. Epub 2016 Mar 16.
J Med Chem. 2016.
PMID: 26938474
Free article.
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Practical purification of hydrophilic fragments and lead/drug-like molecules by reverse phase flash chromatography: tips, tricks and contemporary developments.
Hobbs AN, Young RJ.
Hobbs AN, et al.
Drug Discov Today. 2013 Feb;18(3-4):148-54. doi: 10.1016/j.drudis.2012.09.006. Epub 2012 Sep 20.
Drug Discov Today. 2013.
PMID: 23000487
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