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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: vallee f. 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
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: vallee f. 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 of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.
El-Ahmad Y, Tabart M, Halley F, Certal V, Thompson F, Filoche-Rommé B, Gruss-Leleu F, Muller C, Brollo M, Fabien L, Loyau V, Bertin L, Richepin P, Pilorge F, Desmazeau P, Girardet C, Beccari S, Louboutin A, Lebourg G, Le-Roux J, Terrier C, Vallée F, Steier V, Mathieu M, Rak A, Abecassis PY, Vicat P, Benard T, Bouaboula M, Sun F, Shomali M, Hebert A, Levit M, Cheng H, Courjaud A, Ginesty C, Perrault C, Garcia-Echeverria C, McCort G, Schio L. El-Ahmad Y, et al. Among authors: vallee f. J Med Chem. 2020 Jan 23;63(2):512-528. doi: 10.1021/acs.jmedchem.9b01293. Epub 2019 Nov 27. J Med Chem. 2020. PMID: 31721572
Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.
Vallée F, Carrez C, Pilorge F, Dupuy A, Parent A, Bertin L, Thompson F, Ferrari P, Fassy F, Lamberton A, Thomas A, Arrebola R, Guerif S, Rohaut A, Certal V, Ruxer JM, Gouyon T, Delorme C, Jouanen A, Dumas J, Grépin C, Combeau C, Goulaouic H, Dereu N, Mikol V, Mailliet P, Minoux H. Vallée F, et al. J Med Chem. 2011 Oct 27;54(20):7206-19. doi: 10.1021/jm200784m. Epub 2011 Oct 5. J Med Chem. 2011. PMID: 21972823
Structural basis for human monoglyceride lipase inhibition.
Bertrand T, Augé F, Houtmann J, Rak A, Vallée F, Mikol V, Berne PF, Michot N, Cheuret D, Hoornaert C, Mathieu M. Bertrand T, et al. Among authors: vallee f. J Mol Biol. 2010 Feb 26;396(3):663-73. doi: 10.1016/j.jmb.2009.11.060. Epub 2009 Dec 3. J Mol Biol. 2010. PMID: 19962385
190 results