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Page 1
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.
Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K. Rye CS, et al. Among authors: faulder p. Medchemcomm. 2016 Aug 1;7(8):1580-1586. doi: 10.1039/c6md00159a. Epub 2016 Jun 13. Medchemcomm. 2016. PMID: 27746890 Free PMC article.
Identification and optimization of a novel series of selective PIP5K inhibitors.
Andrews DM, Cartic S, Cosulich S, Divecha N, Faulder P, Flemington V, Kern O, Kettle JG, MacDonald E, McKelvie J, Pike KG, Roberts B, Rowlinson R, Smith JM, Stockley M, Swarbrick ME, Treinies I, Waring MJ. Andrews DM, et al. Among authors: faulder p. Bioorg Med Chem. 2022 Jan 15;54:116557. doi: 10.1016/j.bmc.2021.116557. Epub 2021 Dec 12. Bioorg Med Chem. 2022. PMID: 34922306
Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation.
Winter JJ, Anderson M, Blades K, Brassington C, Breeze AL, Chresta C, Embrey K, Fairley G, Faulder P, Finlay MR, Kettle JG, Nowak T, Overman R, Patel SJ, Perkins P, Spadola L, Tart J, Tucker JA, Wrigley G. Winter JJ, et al. Among authors: faulder p. J Med Chem. 2015 Mar 12;58(5):2265-74. doi: 10.1021/jm501660t. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25695162 Free article.
Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α- but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation.
Waring MJ, Andrews DM, Faulder PF, Flemington V, McKelvie JC, Maman S, Preston M, Raubo P, Robb GR, Roberts K, Rowlinson R, Smith JM, Swarbrick ME, Treinies I, Winter JJ, Wood RJ. Waring MJ, et al. Among authors: faulder pf. Chem Commun (Camb). 2014 May 25;50(40):5388-90. doi: 10.1039/c3cc48391f. Epub 2013 Dec 24. Chem Commun (Camb). 2014. PMID: 24366037
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.
Kettle JG, Brown S, Crafter C, Davies BR, Dudley P, Fairley G, Faulder P, Fillery S, Greenwood H, Hawkins J, James M, Johnson K, Lane CD, Pass M, Pink JH, Plant H, Cosulich SC. Kettle JG, et al. Among authors: faulder p. J Med Chem. 2012 Feb 9;55(3):1261-73. doi: 10.1021/jm201394e. Epub 2012 Jan 27. J Med Chem. 2012. PMID: 22248236
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: faulder p. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome.
Henley ZA, Bax BD, Inglesby LM, Champigny A, Gaines S, Faulder P, Le J, Thomas DA, Washio Y, Baldwin IR. Henley ZA, et al. Among authors: faulder p. ACS Med Chem Lett. 2017 Sep 7;8(10):1093-1098. doi: 10.1021/acsmedchemlett.7b00296. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057057 Free PMC article.
Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.
Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z. Li K, et al. Among authors: faulder p. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11. Bioorg Med Chem Lett. 2013. PMID: 23374866
12 results