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19 results

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Page 1
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: elkins pa. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors.
Sinnamon RH, McDevitt P, Pietrak BL, Leydon VR, Xue Y, Lehr R, Qi H, Burns M, Elkins P, Ward P, Vincentini G, Fisher D, Grimes M, Brandt M, Auger KR, Ho T, Johanson K, Jones CS, Schwartz B, Sweitzer TD, Kirkpatrick RB. Sinnamon RH, et al. Protein Expr Purif. 2010 Oct;73(2):167-76. doi: 10.1016/j.pep.2010.05.002. Epub 2010 May 10. Protein Expr Purif. 2010. PMID: 20457255
Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.
Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF. Seefeld MA, et al. Among authors: elkins pa. J Med Chem. 2003 Apr 24;46(9):1627-35. doi: 10.1021/jm0204035. J Med Chem. 2003. PMID: 12699381
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
Lin H, Yamashita DS, Zeng J, Xie R, Wang W, Nidarmarthy S, Luengo JI, Rhodes N, Knick VB, Choudhry AE, Lai Z, Minthorn EA, Strum SL, Wood ER, Elkins PA, Concha NO, Heerding DA. Lin H, et al. Among authors: elkins pa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):673-8. doi: 10.1016/j.bmcl.2009.11.064. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20006497
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.
Sehon CA, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D. Sehon CA, et al. Among authors: elkins pa. J Med Chem. 2008 Nov 13;51(21):6631-4. doi: 10.1021/jm8005096. Epub 2008 Oct 9. J Med Chem. 2008. PMID: 18842034
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
Stavenger RA, Cui H, Dowdell SE, Franz RG, Gaitanopoulos DE, Goodman KB, Hilfiker MA, Ivy RL, Leber JD, Marino JP Jr, Oh HJ, Viet AQ, Xu W, Ye G, Zhang D, Zhao Y, Jolivette LJ, Head MS, Semus SF, Elkins PA, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Doe CP, Bentley R, Chen ZX, Hu E, Lee D. Stavenger RA, et al. Among authors: elkins pa. J Med Chem. 2007 Jan 11;50(1):2-5. doi: 10.1021/jm060873p. J Med Chem. 2007. PMID: 17201404
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
Su DS, Qu J, Schulz M, Blackledge CW, Yu H, Zeng J, Burgess J, Reif A, Stern M, Nagarajan R, Pappalardi MB, Wong K, Graves AP, Bonnette W, Wang L, Elkins P, Knapp-Reed B, Carson JD, McHugh C, Mohammad H, Kruger R, Luengo J, Heerding DA, Creasy CL. Su DS, et al. ACS Med Chem Lett. 2019 Dec 27;11(2):133-140. doi: 10.1021/acsmedchemlett.9b00493. eCollection 2020 Feb 13. ACS Med Chem Lett. 2019. PMID: 32071679 Free PMC article.
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.
Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D. Knight SD, et al. Among authors: elkins pa. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43. doi: 10.1021/ml900028r. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900173 Free PMC article.
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Yang H, Medeiros PF, Raha K, Elkins P, Lind KE, Lehr R, Adams ND, Burgess JL, Schmidt SJ, Knight SD, Auger KR, Schaber MD, Franklin GJ, Ding Y, DeLorey JL, Centrella PA, Mataruse S, Skinner SR, Clark MA, Cuozzo JW, Evindar G. Yang H, et al. Among authors: elkins p. ACS Med Chem Lett. 2015 Mar 20;6(5):531-6. doi: 10.1021/acsmedchemlett.5b00025. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005528 Free PMC article.
19 results