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Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: eastwood p. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Mapping the kinase domain of Janus Kinase 3.
Adams C, Aldous DJ, Amendola S, Bamborough P, Bright C, Crowe S, Eastwood P, Fenton G, Foster M, Harrison TK, King S, Lai J, Lawrence C, Letallec JP, McCarthy C, Moorcroft N, Page K, Rao S, Redford J, Sadiq S, Smith K, Souness JE, Thurairatnam S, Vine M, Wyman B. Adams C, et al. Among authors: eastwood p. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3105-10. doi: 10.1016/s0960-894x(03)00657-7. Bioorg Med Chem Lett. 2003. PMID: 12941344
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors.
Aiguadé J, Balagué C, Carranco I, Caturla F, Domínguez M, Eastwood P, Esteve C, González J, Lumeras W, Orellana A, Preciado S, Roca R, Vidal L, Vidal B. Aiguadé J, et al. Among authors: eastwood p. Bioorg Med Chem Lett. 2012 May 15;22(10):3431-6. doi: 10.1016/j.bmcl.2012.03.099. Epub 2012 Apr 4. Bioorg Med Chem Lett. 2012. PMID: 22521646
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I.
Alonso JA, Andrés M, Bravo M, Buil MA, Calbet M, Castro J, Eastwood PR, Eichhorn P, Esteve C, Gómez E, González J, Mir M, Petit S, Roberts RS, Vidal B, Vidal L, Vilaseca P, Zanuy M. Alonso JA, et al. Among authors: eastwood pr. Bioorg Med Chem Lett. 2014 Nov 1;24(21):5118-22. doi: 10.1016/j.bmcl.2014.09.005. Epub 2014 Oct 15. Bioorg Med Chem Lett. 2014. PMID: 25437504
Indolin-2-one p38α inhibitors II: Lead optimisation.
Eastwood P, González J, Gómez E, Caturla F, Balagué C, Orellana A, Domínguez M. Eastwood P, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5270-3. doi: 10.1016/j.bmcl.2011.07.033. Epub 2011 Jul 19. Bioorg Med Chem Lett. 2011. PMID: 21813275
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: lead optimization.
Alonso JA, Andrés M, Bravo M, Calbet M, Eastwood PR, Eichhorn P, Esteve C, Ferrer M, Gómez E, González J, Mir M, Moreno I, Petit S, Roberts RS, Sevilla S, Vidal B, Vidal L, Vilaseca P, Zanuy M. Alonso JA, et al. Among authors: eastwood pr. Bioorg Med Chem Lett. 2014 Nov 1;24(21):5123-6. doi: 10.1016/j.bmcl.2014.08.029. Epub 2014 Aug 19. Bioorg Med Chem Lett. 2014. PMID: 25437505
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: the role of a hydrogen-bond acceptor in long receptor residence times.
Alonso JA, Andrés M, Bravo M, Buil MA, Calbet M, Castro J, Eastwood PR, Esteve C, Ferrer M, Forns P, Gómez E, González J, Lozoya E, Mir M, Moreno I, Petit S, Roberts RS, Sevilla S, Vidal B, Vidal L, Vilaseca P. Alonso JA, et al. Among authors: eastwood pr. Bioorg Med Chem Lett. 2014 Nov 1;24(21):5127-33. doi: 10.1016/j.bmcl.2014.08.028. Epub 2014 Aug 19. Bioorg Med Chem Lett. 2014. PMID: 25437506
239 results