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Page 1
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.
Bellenie BR, Cheung KJ, Varela A, Pierrat OA, Collie GW, Box GM, Bright MD, Gowan S, Hayes A, Rodrigues MJ, Shetty KN, Carter M, Davis OA, Henley AT, Innocenti P, Johnson LD, Liu M, de Klerk S, Le Bihan YV, Lloyd MG, McAndrew PC, Shehu E, Talbot R, Woodward HL, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Hoelder S. Bellenie BR, et al. Among authors: innocenti p. J Med Chem. 2020 Apr 23;63(8):4047-4068. doi: 10.1021/acs.jmedchem.9b02076. Epub 2020 Apr 10. J Med Chem. 2020. PMID: 32275432 Free PMC article.
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S. Innocenti P, et al. J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7. J Med Chem. 2016. PMID: 27055065 Free article.
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S. Woodward HL, et al. Among authors: innocenti p. J Med Chem. 2018 Sep 27;61(18):8226-8240. doi: 10.1021/acs.jmedchem.8b00690. Epub 2018 Sep 10. J Med Chem. 2018. PMID: 30199249 Free PMC article.
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.
Solanki S, Innocenti P, Mas-Droux C, Boxall K, Barillari C, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Solanki S, et al. Among authors: innocenti p. J Med Chem. 2011 Mar 24;54(6):1626-39. doi: 10.1021/jm1011726. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366329
Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.
Faisal A, Mak GWY, Gurden MD, Xavier CPR, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, Burke R, vanMontfort RLM, Blagg J, Raynaud FI, Eccles SA, Hoelder S, Linardopoulos S. Faisal A, et al. Among authors: innocenti p. Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23. Br J Cancer. 2017. PMID: 28334731 Free PMC article.
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S. Innocenti P, et al. J Med Chem. 2012 Apr 12;55(7):3228-41. doi: 10.1021/jm201683b. Epub 2012 Mar 23. J Med Chem. 2012. PMID: 22404346 Free PMC article.
High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers.
Anderhub SJ, Mak GW, Gurden MD, Faisal A, Drosopoulos K, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, van Montfort RLM, Raynaud FI, Blagg J, Hoelder S, Eccles SA, Linardopoulos S. Anderhub SJ, et al. Among authors: innocenti p. Mol Cancer Ther. 2019 Oct;18(10):1696-1707. doi: 10.1158/1535-7163.MCT-18-1203. Mol Cancer Ther. 2019. PMID: 31575759
Potent Inhibition of Nicotinamide N-Methyltransferase by Alkene-Linked Bisubstrate Mimics Bearing Electron Deficient Aromatics.
Gao Y, van Haren MJ, Buijs N, Innocenti P, Zhang Y, Sartini D, Campagna R, Emanuelli M, Parsons RB, Jespers W, Gutiérrez-de-Terán H, van Westen GJP, Martin NI. Gao Y, et al. Among authors: innocenti p. J Med Chem. 2021 Sep 9;64(17):12938-12963. doi: 10.1021/acs.jmedchem.1c01094. Epub 2021 Aug 23. J Med Chem. 2021. PMID: 34424711 Free PMC article.
316 results