| Year |
Citation |
Score |
| 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, ... ... Woodward H, 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 |
0.673 |
|
| 2022 |
Zhao Y, Mahy W, Willis NJ, Woodward HL, Steadman D, Bayle ED, Atkinson BN, Sipthorp J, Vecchia L, Ruza RR, Harlos K, Jeganathan F, Constantinou S, Costa A, Kjær S, et al. Structural Analysis and Development of Notum Fragment Screening Hits. Acs Chemical Neuroscience. PMID 35731924 DOI: 10.1021/acschemneuro.2c00325 |
0.374 |
|
| 2022 |
Willis NJ, Mahy W, Sipthorp J, Zhao Y, Woodward HL, Atkinson BN, Bayle ED, Svensson F, Frew S, Jeganathan F, Monaghan A, Benvegnù S, Jolly S, Vecchia L, Ruza RR, et al. Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit. Journal of Medicinal Chemistry. PMID 35536179 DOI: 10.1021/acs.jmedchem.2c00162 |
0.391 |
|
| 2021 |
Bayle ED, Svensson F, Atkinson BN, Steadman D, Willis NJ, Woodward HL, Whiting P, Vincent JP, Fish PV. Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling. Journal of Medicinal Chemistry. PMID 33783220 DOI: 10.1021/acs.jmedchem.0c01974 |
0.301 |
|
| 2020 |
Mahy W, Willis NJ, Zhao Y, Woodward HL, Svensson F, Sipthorp J, Vecchia L, Ruza RR, Hillier J, Kjær S, Frew S, Monaghan A, Bictash M, Salinas PC, Whiting P, et al. 5-Phenyl-1,3,4-oxadiazol-2(3)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit. Journal of Medicinal Chemistry. PMID 33124429 DOI: 10.1021/acs.jmedchem.0c01391 |
0.326 |
|
| 2020 |
Mahy W, Patel M, Steadman D, Woodward H, Atkinson BN, Svensson F, Willis N, Flint A, Papatheodorou D, Zhao Y, Vecchia L, Ruza RR, Hillier J, Frew S, Monaghan A, et al. Screening of a custom-designed acid fragment library identifies 1-phenylpyrroles and 1-phenylpyrrolidines as inhibitors of Notum carboxylesterase activity. Journal of Medicinal Chemistry. PMID 32787107 DOI: 10.1021/acs.jmedchem.0c00660 |
0.388 |
|
| 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, ... ... Woodward HL, 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 |
0.746 |
|
| 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 |
0.752 |
|
| 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 |
0.733 |
|
| 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 |
0.755 |
|
| 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 |
0.783 |
|
| 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 |
0.75 |
|
| 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 |
0.77 |
|
| 2013 |
Vidler LR, Filippakopoulos P, Fedorov O, Picaud S, Martin S, Tomsett M, Woodward H, Brown N, Knapp S, Hoelder S. Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening. Journal of Medicinal Chemistry. 56: 8073-88. PMID 24090311 DOI: 10.1021/Jm4011302 |
0.728 |
|
| 2013 |
Benito-Alifonso D, Jones RA, Tran AT, Woodward H, Smith N, Galan MC. Synthesis of mucin-type O-glycan probes as aminopropyl glycosides. Beilstein Journal of Organic Chemistry. 9: 1867-72. PMID 24062854 DOI: 10.3762/Bjoc.9.218 |
0.316 |
|
| 2013 |
Faisal A, Innocenti P, Westwood I, Naud S, Schmitt J, Hayes A, Mak G, Gurden M, Bavetsias V, Cheung J, Woodward H, Sheldrake P, Atrash B, Burke R, Baker R, et al. Abstract 3242: CCT271850, a novel, selective, highly potent and orally bioavailable Mps1 kinase inhibitor. Cancer Research. 73: 3242-3242. DOI: 10.1158/1538-7445.Am2013-3242 |
0.764 |
|
| 2010 |
Beattie D, Brearley A, Brown Z, Charlton SJ, Cox B, Fairhurst RA, Fozard JR, Gedeck P, Kirkham P, Meja K, Nanson L, Neef J, Oakman H, Spooner G, Taylor RJ, ... ... Woodward H, et al. Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. Bioorganic & Medicinal Chemistry Letters. 20: 1219-24. PMID 20031406 DOI: 10.1016/J.Bmcl.2009.11.131 |
0.319 |
|
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