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22 results

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Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma.
Biggadike K, Ahmed M, Ball DI, Coe DM, Dalmas Wilk DA, Edwards CD, Gibbon BH, Hardy CJ, Hermitage SA, Hessey JO, Hillegas AE, Hughes SC, Lazarides L, Lewell XQ, Lucas A, Mallett DN, Price MA, Priest FM, Quint DJ, Shah P, Sitaram A, Smith SA, Stocker R, Trivedi NA, Tsitoura DC, Weller V. Biggadike K, et al. Among authors: mallett dn. J Med Chem. 2016 Mar 10;59(5):1711-26. doi: 10.1021/acs.jmedchem.5b01647. Epub 2016 Feb 10. J Med Chem. 2016. PMID: 26861551
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN. Henley ZA, et al. J Med Chem. 2020 Jan 23;63(2):638-655. doi: 10.1021/acs.jmedchem.9b01585. Epub 2020 Jan 8. J Med Chem. 2020. PMID: 31855425
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ.
Spencer JA, Baldwin IR, Barton N, Chung CW, Convery MA, Edwards CD, Jamieson C, Mallett DN, Rowedder JE, Rowland P, Thomas DA, Hardy CJ. Spencer JA, et al. Among authors: mallett dn. ACS Med Chem Lett. 2020 Jun 3;11(7):1386-1391. doi: 10.1021/acsmedchemlett.0c00061. eCollection 2020 Jul 9. ACS Med Chem Lett. 2020. PMID: 32676144 Free PMC article.
Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Down K, Amour A, Anderson NA, Barton N, Campos S, Cannons EP, Clissold C, Convery MA, Coward JJ, Doyle K, Duempelfeld B, Edwards CD, Goldsmith MD, Krause J, Mallett DN, McGonagle GA, Patel VK, Rowedder J, Rowland P, Sharpe A, Sriskantharajah S, Thomas DA, Thomson DW, Uddin S, Hamblin JN, Hessel EM. Down K, et al. Among authors: mallett dn. J Med Chem. 2021 Sep 23;64(18):13780-13792. doi: 10.1021/acs.jmedchem.1c01102. Epub 2021 Sep 11. J Med Chem. 2021. PMID: 34510892
Translation of Inhaled Drug Optimization Strategies into Clinical Pharmacokinetics and Pharmacodynamics Using GSK2292767A, a Novel Inhaled Phosphoinositide 3-Kinase δ Inhibitor.
Begg M, Edwards CD, Hamblin JN, Pefani E, Wilson R, Gilbert J, Vitulli G, Mallett D, Morrell J, Hingle MI, Uddin S, Ehtesham F, Marotti M, Harrell A, Newman CF, Fernando D, Clark J, Cahn A, Hessel EM. Begg M, et al. J Pharmacol Exp Ther. 2019 Jun;369(3):443-453. doi: 10.1124/jpet.119.257311. Epub 2019 Apr 2. J Pharmacol Exp Ther. 2019. PMID: 30940692 Clinical Trial.
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