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The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1.
Amaning K, Lowinski M, Vallee F, Steier V, Marcireau C, Ugolini A, Delorme C, Foucalt F, McCort G, Derimay N, Andouche C, Vougier S, Llopart S, Halland N, Rak A. Amaning K, et al. Among authors: rak a. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3620-6. doi: 10.1016/j.bmcl.2013.04.003. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23648182
Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Certal V, et al. Among authors: rak a. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387221
Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844).
Ugolini A, Kenigsberg M, Rak A, Vallée F, Houtmann J, Lowinski M, Capdevila C, Khider J, Albert E, Martinet N, Nemecek C, Grapinet S, Bacqué E, Roesner M, Delaisi C, Calvet L, Bonche F, Semiond D, Egile C, Goulaouic H, Schio L. Ugolini A, et al. Among authors: rak a. J Med Chem. 2016 Aug 11;59(15):7066-74. doi: 10.1021/acs.jmedchem.6b00280. Epub 2016 Jul 13. J Med Chem. 2016. PMID: 27355974
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L. Certal V, et al. Among authors: rak a. J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2. J Med Chem. 2012. PMID: 22524426
222 results