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(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
Pelletier JC, Lundquist JT 4th, Gilbert AM, Alon N, Bex FJ, Bhat BM, Bursavich MG, Coleburn VE, Felix LA, Green DM, Green P, Hauze DB, Kharode YP, Lam HS, Lockhead SR, Magolda RL, Matteo JJ, Mehlmann JF, Milligan C, Murrills RJ, Pirrello J, Selim S, Sharp MC, Unwalla RJ, Vera MD, Wrobel JE, Yaworsky P, Bodine PV. Pelletier JC, et al. Among authors: lockhead sr. J Med Chem. 2009 Nov 26;52(22):6962-5. doi: 10.1021/jm9014197. J Med Chem. 2009. PMID: 19856966
Characterization of HKI-272 covalent binding to human serum albumin.
Wang J, Li-Chan XX, Atherton J, Deng L, Espina R, Yu L, Horwatt P, Ross S, Lockhead S, Ahmad S, Chandrasekaran A, Oganesian A, Scatina J, Mutlib A, Talaat R. Wang J, et al. Among authors: lockhead s. Drug Metab Dispos. 2010 Jul;38(7):1083-93. doi: 10.1124/dmd.110.032292. Epub 2010 Apr 16. Drug Metab Dispos. 2010. PMID: 20400660
Osteogenic effects of a potent Src-over-Abl-selective kinase inhibitor in the mouse.
Murrills RJ, Fukayama S, Boschelli F, Matteo JJ, Owens J, Golas JM, Patel D, Lane G, Liu YB, Carter L, Jussif J, Spaulding V, Wang YD, Boschelli DH, McKew JC, Li XJ, Lockhead S, Milligan C, Kharode YP, Diesl V, Bai Y, Follettie M, Bex FJ, Komm B, Bodine PV. Murrills RJ, et al. Among authors: lockhead s. J Pharmacol Exp Ther. 2012 Mar;340(3):676-87. doi: 10.1124/jpet.111.185793. Epub 2011 Dec 9. J Pharmacol Exp Ther. 2012. PMID: 22171089
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Fensome A, Bender R, Chopra R, Cohen J, Collins MA, Hudak V, Malakian K, Lockhead S, Olland A, Svenson K, Terefenko EA, Unwalla RJ, Wilhelm JM, Wolfrom S, Zhu Y, Zhang Z, Zhang P, Winneker RC, Wrobel J. Fensome A, et al. Among authors: lockhead s. J Med Chem. 2005 Aug 11;48(16):5092-5. doi: 10.1021/jm050358b. J Med Chem. 2005. PMID: 16078826
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z. Zhang P, et al. Among authors: lockhead s. Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. doi: 10.1016/j.bmc.2007.07.011. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17681796