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Page 1
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. Deaton DN, et al. Among authors: peckham ge. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. Bioorg Med Chem. 2019. PMID: 30858025
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: peckham ge. 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
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: peckham ge. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Cheung M, Harris PA, Badiang JG, Peckham GE, Chamberlain SD, Alberti MJ, Jung DK, Harris SS, Bramson NH, Epperly AH, Stimpson SA, Peel MR. Cheung M, et al. Among authors: peckham ge. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5428-30. doi: 10.1016/j.bmcl.2008.09.040. Epub 2008 Sep 12. Bioorg Med Chem Lett. 2008. PMID: 18818075
Novel benzimidazole-based MCH R1 antagonists.
Carpenter AJ, Al-Barazanji KA, Barvian KK, Bishop MJ, Britt CS, Cooper JP, Goetz AS, Grizzle MK, Hertzog DL, Ignar DM, Morgan RO, Peckham GE, Speake JD, Swain WR. Carpenter AJ, et al. Among authors: peckham ge. Bioorg Med Chem Lett. 2006 Oct 1;16(19):4994-5000. doi: 10.1016/j.bmcl.2006.07.054. Epub 2006 Aug 9. Bioorg Med Chem Lett. 2006. PMID: 16904318
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.
Katamreddy SR, Carpenter AJ, Ammala CE, Boros EE, Brashear RL, Briscoe CP, Bullard SR, Caldwell RD, Conlee CR, Croom DK, Hart SM, Heyer DO, Johnson PR, Kashatus JA, Minick DJ, Peckham GE, Ross SA, Roller SG, Samano VA, Sauls HR, Tadepalli SM, Thompson JB, Xu Y, Way JM. Katamreddy SR, et al. Among authors: peckham ge. J Med Chem. 2012 Dec 27;55(24):10972-94. doi: 10.1021/jm301404a. Epub 2012 Dec 12. J Med Chem. 2012. PMID: 23214471
Pyrazolo[1,5-a]pyridines as p38 kinase inhibitors.
Stevens KL, Jung DK, Alberti MJ, Badiang JG, Peckham GE, Veal JM, Cheung M, Harris PA, Chamberlain SD, Peel MR. Stevens KL, et al. Among authors: peckham ge. Org Lett. 2005 Oct 13;7(21):4753-6. doi: 10.1021/ol0519745. Org Lett. 2005. PMID: 16209527