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94 results

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Page 1
Assessing atropisomer axial chirality in drug discovery and development.
Laplante SR, D Fader L, Fandrick KR, Fandrick DR, Hucke O, Kemper R, Miller SP, Edwards PJ. Laplante SR, et al. Among authors: kemper r. J Med Chem. 2011 Oct 27;54(20):7005-22. doi: 10.1021/jm200584g. Epub 2011 Sep 15. J Med Chem. 2011. PMID: 21848318 Review. No abstract available.
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
Huber JD, Bentzien J, Boyer SJ, Burke J, De Lombaert S, Eickmeier C, Guo X, Haist JV, Hickey ER, Kaplita P, Karmazyn M, Kemper R, Kennedy CA, Kirrane T, Madwed JB, Mainolfi E, Nagaraja N, Soleymanzadeh F, Swinamer A, Eldrup AB. Huber JD, et al. Among authors: kemper r. J Med Chem. 2012 Aug 23;55(16):7114-40. doi: 10.1021/jm300601d. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22803959
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Horan JC, Kuzmich D, Liu P, DiSalvo D, Lord J, Mao C, Hopkins TD, Yu H, Harcken C, Betageri R, Hill-Drzewi M, Patenaude L, Patel M, Fletcher K, Terenzzio D, Linehan B, Xia H, Patel M, Studwell D, Miller C, Hickey E, Levin JI, Smith D, Kemper RA, Modis LK, Bannen LC, Chan DS, Mac MB, Ng S, Wang Y, Xu W, Lemieux RM. Horan JC, et al. Among authors: kemper ra. Bioorg Med Chem Lett. 2016 Jan 15;26(2):466-471. doi: 10.1016/j.bmcl.2015.11.090. Epub 2015 Nov 26. Bioorg Med Chem Lett. 2016. PMID: 26687487
Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.
Come JH, Senter TJ, Clark MP, Court JJ, Gale-Day Z, Gu W, Krueger E, Liang J, Morris M, Nanthakumar S, O'Dowd H, Maltais F, Iyer G, Andreassi J, Boucher C, Considine T, Moody CS, Taylor W, Mohanty AK, Huang Y, Zuccola H, Coll J, Bonanno KC, Gagnon KJ, Gan L, Lu F, Gao H, Chakilam A, Engtrakul J, Song B, Crawford D, Doyle E, Kramer T, Vought B, Phillips J, Kemper R, Sanders M, Swett R, Furey B, Winquist R, Bunnage ME, Jackson KL, Charifson PS, Magavi SS. Come JH, et al. Among authors: kemper r. J Med Chem. 2021 Dec 23;64(24):17753-17776. doi: 10.1021/acs.jmedchem.1c00944. Epub 2021 Nov 8. J Med Chem. 2021. PMID: 34748351
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Boyd MJ, Collier PN, Clark MP, Deng H, Kesavan S, Ronkin SM, Waal N, Wang J, Cao J, Li P, Come J, Davies I, Duffy JP, Cochran JE, Court JJ, Chandupatla K, Jackson KL, Maltais F, O'Dowd H, Boucher C, Considine T, Taylor WP, Gao H, Chakilam A, Engtrakul J, Crawford D, Doyle E, Phillips J, Kemper R, Swett R, Empfield J, Bunnage ME, Charifson PS, Magavi SS. Boyd MJ, et al. Among authors: kemper r. J Med Chem. 2021 Dec 23;64(24):17777-17794. doi: 10.1021/acs.jmedchem.1c00948. Epub 2021 Dec 6. J Med Chem. 2021. PMID: 34871500
Discovery of MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction.
Reutershan MH, Machacek MR, Altman MD, Bogen S, Cai M, Cammarano C, Chen D, Christopher M, Cryan J, Daublain P, Fradera X, Geda P, Goldenblatt P, Hill AD, Kemper RA, Kutilek V, Li C, Martinez M, McCoy M, Nair L, Pan W, Thompson CF, Scapin G, Shizuka M, Spatz ML, Steinhuebel D, Sun B, Voss ME, Wang X, Yang L, Yeh TC, Dussault I, Marshall CG, Trotter BW. Reutershan MH, et al. Among authors: kemper ra. J Med Chem. 2021 Nov 11;64(21):16213-16241. doi: 10.1021/acs.jmedchem.1c01524. Epub 2021 Oct 29. J Med Chem. 2021. PMID: 34714078
Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.
Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD. Methot JL, et al. Among authors: kemper r. J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22. J Med Chem. 2019. PMID: 30986068
A cross-industry collaboration to assess if acute oral toxicity (Q)SAR models are fit-for-purpose for GHS classification and labelling.
Bercu J, Masuda-Herrera MJ, Trejo-Martin A, Hasselgren C, Lord J, Graham J, Schmitz M, Milchak L, Owens C, Lal SH, Robinson RM, Whalley S, Bellion P, Vuorinen A, Gromek K, Hawkins WA, van de Gevel I, Vriens K, Kemper R, Naven R, Ferrer P, Myatt GJ. Bercu J, et al. Among authors: kemper r. Regul Toxicol Pharmacol. 2021 Mar;120:104843. doi: 10.1016/j.yrtph.2020.104843. Epub 2020 Dec 17. Regul Toxicol Pharmacol. 2021. PMID: 33340644 Free PMC article.
Evaluation of a statistics-based Ames mutagenicity QSAR model and interpretation of the results obtained.
Barber C, Cayley A, Hanser T, Harding A, Heghes C, Vessey JD, Werner S, Weiner SK, Wichard J, Giddings A, Glowienke S, Parenty A, Brigo A, Spirkl HP, Amberg A, Kemper R, Greene N. Barber C, et al. Among authors: kemper r. Regul Toxicol Pharmacol. 2016 Apr;76:7-20. doi: 10.1016/j.yrtph.2015.12.006. Epub 2015 Dec 18. Regul Toxicol Pharmacol. 2016. PMID: 26708083
94 results