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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V. Le Bihan YV, et al. Among authors: mok ny. Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17. Eur J Med Chem. 2019. PMID: 31158747 Free PMC article.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: mok ny. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.
Harrison JR, Brand S, Smith V, Robinson DA, Thompson S, Smith A, Davies K, Mok N, Torrie LS, Collie I, Hallyburton I, Norval S, Simeons FRC, Stojanovski L, Frearson JA, Brenk R, Wyatt PG, Gilbert IH, Read KD. Harrison JR, et al. J Med Chem. 2018 Sep 27;61(18):8374-8389. doi: 10.1021/acs.jmedchem.8b00884. Epub 2018 Sep 12. J Med Chem. 2018. PMID: 30207721 Free PMC article.
Privileged Structures and Polypharmacology within and between Protein Families.
Meyers J, Chessum NEA, Ali S, Mok NY, Wilding B, Pasqua AE, Rowlands M, Tucker MJ, Evans LE, Rye CS, O'Fee L, Le Bihan YV, Burke R, Carter M, Workman P, Blagg J, Brown N, van Montfort RLM, Jones K, Cheeseman MD. Meyers J, et al. Among authors: mok ny. ACS Med Chem Lett. 2018 Nov 16;9(12):1199-1204. doi: 10.1021/acsmedchemlett.8b00364. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613326 Free PMC article.
Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease.
Colombano G, Caldwell JJ, Matthews TP, Bhatia C, Joshi A, McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R, Collins I. Colombano G, et al. Among authors: mok ny. J Med Chem. 2019 Mar 14;62(5):2447-2465. doi: 10.1021/acs.jmedchem.8b01721. Epub 2019 Mar 5. J Med Chem. 2019. PMID: 30779566 Free PMC article.
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies.
Pasqua AE, Sharp SY, Chessum NEA, Hayes A, Pellegrino L, Tucker MJ, Miah A, Wilding B, Evans LE, Rye CS, Mok NY, Liu M, Henley AT, Gowan S, De Billy E, Te Poele R, Powers M, Eccles SA, Clarke PA, Raynaud FI, Workman P, Jones K, Cheeseman MD. Pasqua AE, et al. Among authors: mok ny. J Med Chem. 2023 Apr 27;66(8):5907-5936. doi: 10.1021/acs.jmedchem.3c00156. Epub 2023 Apr 5. J Med Chem. 2023. PMID: 37017629 Free PMC article.
On the origins of three-dimensionality in drug-like molecules.
Meyers J, Carter M, Mok NY, Brown N. Meyers J, et al. Among authors: mok ny. Future Med Chem. 2016 Sep;8(14):1753-67. doi: 10.4155/fmc-2016-0095. Epub 2016 Aug 30. Future Med Chem. 2016. PMID: 27572621 Free PMC article.
17 results