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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: smith jm. Chem Commun (Camb). 2014 May 25;50(40):5388-90. doi: 10.1039/c3cc48391f. Epub 2013 Dec 24. Chem Commun (Camb). 2014. PMID: 24366037
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J. Boyd S, et al. Among authors: smith jm. J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13. J Med Chem. 2015. PMID: 25849762
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.
Finlay MRV, Anderton M, Bailey A, Boyd S, Brookfield J, Cairnduff C, Charles M, Cheasty A, Critchlow SE, Culshaw J, Ekwuru T, Hollingsworth I, Jones N, Leroux F, Littleson M, McCarron H, McKelvie J, Mooney L, Nissink JWM, Perkins D, Powell S, Quesada MJ, Raubo P, Sabin V, Smith J, Smith PD, Stark A, Ting A, Wang P, Wilson Z, Winter-Holt JJ, Wood JM, Wrigley GL, Yu G, Zhang P. Finlay MRV, et al. Among authors: smith j, smith pd. J Med Chem. 2019 Jul 25;62(14):6540-6560. doi: 10.1021/acs.jmedchem.9b00260. Epub 2019 Jul 16. J Med Chem. 2019. PMID: 31199640
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. Among authors: smith jm. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: smith jm. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
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: smith jm. 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
Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
De Fusco C, Schimpl M, Börjesson U, Cheung T, Collie I, Evans L, Narasimhan P, Stubbs C, Vazquez-Chantada M, Wagner DJ, Grondine M, Sanders MG, Tentarelli S, Underwood E, Argyrou A, Smith JM, Lynch JT, Chiarparin E, Robb G, Bagal SK, Scott JS. De Fusco C, et al. Among authors: smith jm. J Med Chem. 2021 May 27;64(10):6814-6826. doi: 10.1021/acs.jmedchem.1c00067. Epub 2021 Apr 26. J Med Chem. 2021. PMID: 33900758 Free article.
Development of a Series of Pyrrolopyridone MAT2A Inhibitors.
Atkinson SJ, Bagal SK, Argyrou A, Askin S, Cheung T, Chiarparin E, Coen M, Collie IT, Dale IL, De Fusco C, Dillman K, Evans L, Feron LJ, Foster AJ, Grondine M, Kantae V, Lamont GM, Lamont S, Lynch JT, Nilsson Lill S, Robb GR, Saeh J, Schimpl M, Scott JS, Smith J, Srinivasan B, Tentarelli S, Vazquez-Chantada M, Wagner D, Walsh JJ, Watson D, Williamson B. Atkinson SJ, et al. J Med Chem. 2024 Mar 28;67(6):4541-4559. doi: 10.1021/acs.jmedchem.3c01860. Epub 2024 Mar 11. J Med Chem. 2024. PMID: 38466661
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y. Kettle JG, et al. Among authors: smith jm, smith a. J Med Chem. 2018 Oct 11;61(19):8797-8810. doi: 10.1021/acs.jmedchem.8b00938. Epub 2018 Sep 24. J Med Chem. 2018. PMID: 30204441
1,973 results