Year |
Citation |
Score |
2023 |
Liu M, Mirza A, McAndrew PC, Thapaliya A, Pierrat OA, Stubbs M, Hahner T, Chessum NEA, Innocenti P, Caldwell J, Cheeseman MD, Bellenie BR, van Montfort RLM, Newton GK, Burke R, et al. Determination of Ligand-Binding Affinity () Using Transverse Relaxation Rate () in the Ligand-Observed H NMR Experiment and Applications to Fragment-Based Drug Discovery. Journal of Medicinal Chemistry. PMID 37467168 DOI: 10.1021/acs.jmedchem.3c00758 |
0.65 |
|
2022 |
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, ... ... Innocenti P, et al. Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays. Scientific Reports. 12: 18633. PMID 36329085 DOI: 10.1038/s41598-022-23264-z |
0.706 |
|
2021 |
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. Potent Inhibition of Nicotinamide -Methyltransferase by Alkene-Linked Bisubstrate Mimics Bearing Electron Deficient Aromatics. Journal of Medicinal Chemistry. PMID 34424711 DOI: 10.1021/acs.jmedchem.1c01094 |
0.444 |
|
2020 |
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, et al. Achieving Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders. Journal of Medicinal Chemistry. PMID 32275432 DOI: 10.1021/Acs.Jmedchem.9B02076 |
0.763 |
|
2019 |
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, et al. High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers. Molecular Cancer Therapeutics. 18: 1696-1707. PMID 31575759 DOI: 10.1158/1535-7163.Mct-18-1203 |
0.769 |
|
2018 |
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, et al. 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 N-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722). Journal of Medicinal Chemistry. PMID 30199249 DOI: 10.1021/Acs.Jmedchem.8B00690 |
0.752 |
|
2017 |
Faisal A, Mak GW, Gurden MD, Xavier CP, 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, et al. Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy. British Journal of Cancer. PMID 28334731 DOI: 10.1038/Bjc.2017.75 |
0.77 |
|
2016 |
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, et al. Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. Journal of Medicinal Chemistry. PMID 27055065 DOI: 10.1021/Acs.Jmedchem.5B01811 |
0.792 |
|
2015 |
Tucker ER, Danielson LS, Innocenti P, Chesler L. Tackling Crizotinib Resistance: The Pathway from Drug Discovery to the Pediatric Clinic. Cancer Research. 75: 2770-4. PMID 26122839 DOI: 10.1158/0008-5472.Can-14-3817 |
0.432 |
|
2015 |
Innocenti P, Woodward H, O'Fee L, Hoelder S. Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines. Organic & Biomolecular Chemistry. 13: 893-904. PMID 25407826 DOI: 10.1039/C4Ob02238F |
0.765 |
|
2015 |
Innocenti P, Woodward H, Cheung KJ, Naud S, Solanki S, Westwood IM, Faisal A, Hayes A, Schmitt J, Baker R, Matijssen B, Burke R, Eccles SA, Raynaud FI, Linardopoulos S, et al. Abstract 3642: Structure enabled design of inhibitors of the mitotic kinase MPS1 Cancer Research. 75: 3642-3642. DOI: 10.1158/1538-7445.Am2015-3642 |
0.784 |
|
2012 |
Wylie L, Innocenti P, Whelligan DK, Hoelder S. Synthesis of amino-substituted indoles using the Bartoli reaction. Organic & Biomolecular Chemistry. 10: 4441-7. PMID 22565609 DOI: 10.1039/C2Ob25256B |
0.625 |
|
2012 |
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. Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. Journal of Medicinal Chemistry. 55: 3228-41. PMID 22404346 DOI: 10.1021/Jm201683B |
0.754 |
|
2012 |
Faisal A, Naud S, Schmitt J, Westwood I, Hayes A, Gurden M, Bavetsias V, Berry T, Mak G, Innocenti P, Cheung J, Sheldrake P, Atrash B, Sun C, Matijssen B, et al. Abstract 1817: Characterisation of CCT251455, a novel, selective and highly potent Mps1 kinase inhibitor Cancer Research. 72: 1817-1817. DOI: 10.1158/1538-7445.Am2012-1817 |
0.762 |
|
2011 |
Solanki S, Innocenti P, Mas-Droux C, Boxall K, Barillari C, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. 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. Journal of Medicinal Chemistry. 54: 1626-39. PMID 21366329 DOI: 10.1021/Jm1011726 |
0.729 |
|
2005 |
Maffucci T, Piccolo E, Cumashi A, Iezzi M, Riley AM, Saiardi A, Godage HY, Rossi C, Broggini M, Iacobelli S, Potter BV, Innocenti P, Falasca M. Inhibition of the phosphatidylinositol 3-kinase/Akt pathway by inositol pentakisphosphate results in antiangiogenic and antitumor effects. Cancer Research. 65: 8339-49. PMID 16166311 DOI: 10.1158/0008-5472.Can-05-0121 |
0.416 |
|
2004 |
Piccolo E, Vignati S, Maffucci T, Innominato PF, Riley AM, Potter BV, Pandolfi PP, Broggini M, Iacobelli S, Innocenti P, Falasca M. Inositol pentakisphosphate promotes apoptosis through the PI 3-K/Akt pathway. Oncogene. 23: 1754-65. PMID 14755253 DOI: 10.1038/Sj.Onc.1207296 |
0.422 |
|
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