| Year |
Citation |
Score |
| 2020 |
Moore AS, Faisal A, Mak GWY, Miraki-Moud F, Bavetsias V, Valenti M, Box G, Hallsworth A, de Haven Brandon A, Xavier CPR, Stronge R, Pearson ADJ, Blagg J, Raynaud FI, Chopra R, et al. Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736. Blood Advances. 4: 1478-1491. PMID 32282883 DOI: 10.1182/Bloodadvances.2019000986 |
0.359 |
|
| 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, ... ... Blagg J, 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 |
0.365 |
|
| 2019 |
Romo-Morales A, Aladowicz E, Blagg J, Gatz SA, Shipley JM. Catalytic inhibition of KDM1A in Ewing sarcoma is insufficient as a therapeutic strategy. Pediatric Blood & Cancer. e27888. PMID 31207107 DOI: 10.1002/Pbc.27888 |
0.326 |
|
| 2019 |
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, ... ... Blagg J, et al. 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. European Journal of Medicinal Chemistry. 177: 316-337. PMID 31158747 DOI: 10.1016/J.Ejmech.2019.05.041 |
0.729 |
|
| 2019 |
Gilburt JAH, Girvan P, Blagg J, Ying L, Dodson CA. Ligand discrimination between active and inactive activation loop conformations of Aurora-A kinase is unmodified by phosphorylation. Chemical Science. 10: 4069-4076. PMID 31015948 DOI: 10.1039/C8Sc03669A |
0.333 |
|
| 2019 |
Wood F, Shepherd S, Hayes A, Liu M, Grira K, Mok Y, Linardopoulos S, Bavetsias V, Atrash B, Faisal A, Blagg J, Raynaud FI. Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation For Pharmaceutical Sciences. PMID 30953752 DOI: 10.1016/J.Ejps.2019.04.004 |
0.317 |
|
| 2019 |
Calpena E, Hervieu A, Kaserer T, Swagemakers SMA, Goos JAC, Popoola O, Ortiz-Ruiz MJ, Barbaro-Dieber T, Bownass L, Brilstra EH, Brimble E, Foulds N, Grebe TA, Harder AVE, Lees MM, ... ... Blagg J, et al. De Novo Missense Substitutions in the Gene Encoding CDK8, a Regulator of the Mediator Complex, Cause a Syndromic Developmental Disorder. American Journal of Human Genetics. PMID 30905399 DOI: 10.1016/J.Ajhg.2019.02.006 |
0.31 |
|
| 2019 |
Sharifnia T, Wawer MJ, Chen T, Huang QY, Weir BA, Sizemore A, Lawlor MA, Goodale A, Cowley GS, Vazquez F, Ott CJ, Francis JM, Sassi S, Cogswell P, Sheppard HE, ... ... Blagg J, et al. Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nature Medicine. PMID 30664779 DOI: 10.1038/S41591-018-0312-3 |
0.345 |
|
| 2018 |
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, et al. Privileged Structures and Polypharmacology within and between Protein Families. Acs Medicinal Chemistry Letters. 9: 1199-1204. PMID 30613326 DOI: 10.1021/Acsmedchemlett.8B00364 |
0.367 |
|
| 2018 |
Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs A, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, ... ... Blagg J, et al. Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Angewandte Chemie (International Ed. in English). PMID 30431220 DOI: 10.1002/Anie.201810179 |
0.533 |
|
| 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, ... ... Blagg J, 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 |
0.392 |
|
| 2018 |
Popoola OO, Ortiz-Ruiz MJ, Mitsopoulos K, Mallinger A, Te-Poele R, Schiemann K, Workman P, Wienke D, Blagg J, Eccles SA, Clarke PA. Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer Molecular Cancer Therapeutics. 17. DOI: 10.1158/1535-7163.Targ-17-A187 |
0.374 |
|
| 2017 |
Whittaker SR, Barlow C, Martin MP, Mancusi C, Wagner S, Self A, Barrie E, Te Poele R, Sharp S, Brown N, Wilson S, Jackson W, Fischer PM, Clarke PA, Walton MI, ... ... Blagg J, et al. Molecular profiling and combinatorial activity of CCT068127: A potent CDK2 and CDK9 inhibitor. Molecular Oncology. PMID 29063678 DOI: 10.1002/1878-0261.12148 |
0.385 |
|
| 2017 |
Gilburt JAH, Sarkar H, Sheldrake P, Blagg J, Ying L, Dodson C. Dynamic Equilibrium of the Aurora-A Kinase Activation Loop Revealed by Single Molecule Spectroscopy. Angewandte Chemie (International Ed. in English). PMID 28700101 DOI: 10.1002/Anie.201704654 |
0.325 |
|
| 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, ... ... Blagg J, 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 |
0.352 |
|
| 2017 |
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, ... ... Blagg J, et al. Assessing histone demethylase inhibitors in cells: lessons learned. Epigenetics & Chromatin. 10: 9. PMID 28265301 DOI: 10.1186/S13072-017-0116-6 |
0.501 |
|
| 2017 |
Woodward HL, Innocenti P, Cheung KJ, Naud S, Hayes A, Henley AT, Faisal A, Mak G, Box G, Westwood IM, Carter M, Valenti M, Brandon ADH, O’Fee L, Saville H, ... ... Blagg J, et al. Abstract 193: Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidate Cancer Research. 77: 193-193. DOI: 10.1158/1538-7445.Am2017-193 |
0.445 |
|
| 2017 |
Clarke PA, Ortiz-Ruiz M, Poele RT, Adeniji-Popoola O, Box G, Esdar C, Ewan K, Gowan S, Brandon ADH, Hewitt P, Kaufmann W, Mallinger A, Raynaud F, Rohdich F, Schiemann K, ... ... Blagg J, et al. Abstract 129: Assessing the mechanism and therapeutic potential of modulators of the human mediator complex-associated protein kinases CDK8 and CDK19 Cancer Research. 77: 129-129. DOI: 10.1158/1538-7445.Am2017-129 |
0.319 |
|
| 2016 |
Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, ... ... Blagg J, et al. Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases. Elife. 5. PMID 27935476 DOI: 10.7554/Elife.20722 |
0.406 |
|
| 2016 |
Rodgers UR, Lanyon-Hogg T, Masumoto N, Ritzefeld M, Burke R, Blagg J, Magee AI, Tate EW. Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. Acs Chemical Biology. PMID 27779865 DOI: 10.1021/Acschembio.6B00896 |
0.385 |
|
| 2016 |
Hayes A, Mok NY, Liu M, Thai C, Henley AT, Atrash B, Lanigan RM, Sejberg J, Le Bihan YV, Bavetsias V, Blagg J, Raynaud FI. Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution. Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 1-23. PMID 27618572 DOI: 10.1080/00498254.2016.1230245 |
0.373 |
|
| 2016 |
Czodrowski P, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Ortiz Ruiz MJ, Schneider R, Raynaud FI, Clarke PA, Musil D, Schwarz D, Dale TC, ... ... Blagg J, et al. Structure-based optimization of potent, selective and orally bioavailable CDK8 inhibitors discovered by high throughput screening. Journal of Medicinal Chemistry. PMID 27490956 DOI: 10.1021/Acs.Jmedchem.6B00597 |
0.434 |
|
| 2016 |
Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, ... ... Blagg J, et al. 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. Acs Medicinal Chemistry Letters. 7: 573-8. PMID 27326329 DOI: 10.1021/Acsmedchemlett.6B00022 |
0.747 |
|
| 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, ... ... Blagg J, 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 |
0.399 |
|
| 2016 |
Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J. Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. Bioorganic & Medicinal Chemistry Letters. 26: 1443-51. PMID 26852363 DOI: 10.1016/J.Bmcl.2016.01.062 |
0.411 |
|
| 2016 |
Mallinger A, Schiemann K, Rink C, Stieber F, Calderini M, Crumpler S, Stubbs M, Adeniji-Popoola O, Poeschke O, Busch M, Czodrowski P, Musil D, Schwarz D, Ortiz-Ruiz MJ, Schneider R, ... ... Blagg J, et al. Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. Journal of Medicinal Chemistry. PMID 26796641 DOI: 10.1021/Acs.Jmedchem.5B01685 |
0.422 |
|
| 2016 |
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, ... ... Blagg J, et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26741168 DOI: 10.1021/Acs.Jmedchem.5B01635 |
0.692 |
|
| 2016 |
Ruiz MJO, Popoola O, Mallinger A, Gowan S, Court W, Box G, Valenti M, Brandon ADH, Te-Poele R, Workman P, Schiemann K, Esdar C, Wienke D, Blagg J, Clarke P, et al. Abstract 4355: Elucidation of the different roles of CDK8 and CDK19 in colorectal cancer (CRC) using CRISPR gene editing technology Cancer Research. 76: 4355-4355. DOI: 10.1158/1538-7445.Am2016-4355 |
0.404 |
|
| 2016 |
Popoola OO, Samant R, Ortiz-Ruiz M, Mallinger A, Court W, Hobbs S, Te-Poele R, Stubbs M, Burke R, Esdar C, Schiemann K, Wienke D, Eccles S, Blagg J, Workman P, et al. Abstract 3869: Phosphoproteomic-based identification of CDK8/CDK19 substrates in colorectal cancer Cancer Research. 76: 3869-3869. DOI: 10.1158/1538-7445.Am2016-3869 |
0.39 |
|
| 2016 |
Clarke P, Esdar C, Mallinger A, Schiemann K, Waalboer D, Crumpler S, Rink C, Stieber F, Calderini M, Adeniji-Popoola O, Ortiz-Ruiz M, Samant RS, Czodrowski P, Musil D, Schwarz D, ... ... Blagg J, et al. Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential Cancer Research. 76: 3025-3025. DOI: 10.1158/1538-7445.Am2016-3025 |
0.425 |
|
| 2015 |
Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, ... ... Blagg J, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nature Chemical Biology. PMID 26502155 DOI: 10.1038/Nchembio.1952 |
0.376 |
|
| 2015 |
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, et al. Corrigendum: The promise and peril of chemical probes. Nature Chemical Biology. 11: 887. PMID 26485080 DOI: 10.1038/Nchembio1115-887C |
0.394 |
|
| 2015 |
Bavetsias V, Pérez-Fuertes Y, McIntyre PJ, Atrash B, Kosmopoulou M, O'Fee L, Burke R, Sun C, Faisal A, Bush K, Avery S, Henley A, Raynaud FI, Linardopoulos S, Bayliss R, ... Blagg J, et al. 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent. Bioorganic & Medicinal Chemistry Letters. 25: 4203-9. PMID 26296477 DOI: 10.1016/J.Bmcl.2015.08.003 |
0.371 |
|
| 2015 |
Gurden MD, Westwood IM, Faisal A, Naud S, Cheung KM, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Van Montfort RL, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Research. 75: 3340-54. PMID 26202014 DOI: 10.1158/0008-5472.Can-14-3272 |
0.317 |
|
| 2015 |
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, et al. The promise and peril of chemical probes. Nature Chemical Biology. 11: 536-41. PMID 26196764 DOI: 10.1038/Nchembio.1867 |
0.379 |
|
| 2015 |
Linardopoulos S, Blagg J. Aurora kinase inhibition: a new light in the sky? Journal of Medicinal Chemistry. 58: 5186-8. PMID 26111271 DOI: 10.1021/Acs.Jmedchem.5B00918 |
0.354 |
|
| 2015 |
Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, ... ... Blagg J, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. Journal of Medicinal Chemistry. 58: 1717-35. PMID 25680029 DOI: 10.1021/Jm501436M |
0.346 |
|
| 2015 |
Gurden MD, Westwood I, Faisal A, Naud S, Cheung J, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Montfort RV, et al. Abstract 5450: Naturally occurring mutations in the MPS1 gene predispose cells to kinase inhibitor drug-resistance Cancer Research. 75: 5450-5450. DOI: 10.1158/1538-7445.Am2015-5450 |
0.335 |
|
| 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, ... Blagg J, 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 |
0.411 |
|
| 2015 |
Clarke PA, Dale T, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz M, Mallinger A, Ewan K, Poele Rt, Gowan S, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J. Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology Molecular Cancer Therapeutics. 14. DOI: 10.1158/1535-7163.Targ-15-Pr02 |
0.441 |
|
| 2014 |
Blagg J, Workman P. Chemical biology approaches to target validation in cancer. Current Opinion in Pharmacology. 17: 87-100. PMID 25175311 DOI: 10.1016/J.Coph.2014.07.007 |
0.301 |
|
| 2014 |
Rowan F, Richards M, Widya M, Bayliss R, Blagg J. Diverse functionalization of Aurora-A kinase at specified surface and buried sites by native chemical modification. Plos One. 9: e103935. PMID 25093837 DOI: 10.1371/Journal.Pone.0103935 |
0.317 |
|
| 2014 |
Walters ZS, Villarejo-Balcells B, Olmos D, Buist TW, Missiaglia E, Allen R, Al-Lazikani B, Garrett MD, Blagg J, Shipley J. JARID2 is a direct target of the PAX3-FOXO1 fusion protein and inhibits myogenic differentiation of rhabdomyosarcoma cells. Oncogene. 33: 1148-57. PMID 23435416 DOI: 10.1038/Onc.2013.46 |
0.325 |
|
| 2013 |
Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, ... ... Blagg J, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). Journal of Medicinal Chemistry. 56: 10045-65. PMID 24256217 DOI: 10.1021/Jm401395S |
0.442 |
|
| 2013 |
Bavetsias V, Faisal A, Crumpler S, Brown N, Kosmopoulou M, Joshi A, Atrash B, Pérez-Fuertes Y, Schmitt JA, Boxall KJ, Burke R, Sun C, Avery S, Bush K, Henley A, ... ... Blagg J, et al. Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells. Journal of Medicinal Chemistry. 56: 9122-35. PMID 24195668 DOI: 10.1021/Jm401115G |
0.414 |
|
| 2013 |
Rowan FC, Richards M, Bibby RA, Thompson A, Bayliss R, Blagg J. Insights into Aurora-A kinase activation using unnatural amino acids incorporated by chemical modification. Acs Chemical Biology. 8: 2184-91. PMID 23924325 DOI: 10.1021/Cb400425T |
0.319 |
|
| 2013 |
Silva-Santisteban MC, Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, et al. Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2. Plos One. 8: e65689. PMID 23776527 DOI: 10.1371/Journal.Pone.0065689 |
0.389 |
|
| 2013 |
Langdon SR, Westwood IM, van Montfort RL, Brown N, Blagg J. Scaffold-focused virtual screening: prospective application to the discovery of TTK inhibitors. Journal of Chemical Information and Modeling. 53: 1100-12. PMID 23672464 DOI: 10.1021/Ci400100C |
0.359 |
|
| 2013 |
Macdonald J, Oldfield V, Bavetsias V, Blagg J. Regioselective C2-arylation of imidazo[4,5-b]pyridines. Organic & Biomolecular Chemistry. 11: 2335-47. PMID 23429655 DOI: 10.1039/C3Ob27477B |
0.3 |
|
| 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, ... ... Blagg J, 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 |
0.399 |
|
| 2013 |
Stowell A, Hamilton N, Hitchin J, Blagg J, Burke R, Burns S, Cockerill MJ, Fairweather E, Hutton C, Jordan A, Mould D, Thomson G, Waddell I, Ogilvie D. Abstract B98: Development and evaluation of selective, reversible LSD1 inhibitors from fragment startpoints. Molecular Cancer Therapeutics. 12. DOI: 10.1158/1535-7163.Targ-13-B98 |
0.443 |
|
| 2013 |
Hitchin JR, Blagg J, Burke R, Burns S, Cockerill MJ, Fairweather EE, Hutton C, Jordan AM, McAndrew C, Mirza A, Mould D, Thomson GJ, Waddell I, Ogilvie DJ. Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments Medchemcomm. 4: 1513-1522. DOI: 10.1039/C3Md00226H |
0.426 |
|
| 2012 |
Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, ... ... Blagg J, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. Journal of Medicinal Chemistry. 55: 8721-34. PMID 23043539 DOI: 10.1021/Jm300952S |
0.374 |
|
| 2012 |
Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, et al. Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia. 26: 1462-70. PMID 22354205 DOI: 10.1038/Leu.2012.52 |
0.338 |
|
| 2012 |
Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW, Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L, Blagg J, Workman P, et al. Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. Plos One. 7: e28568. PMID 22253692 DOI: 10.1371/Journal.Pone.0028568 |
0.355 |
|
| 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, ... ... Blagg J, 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 |
0.383 |
|
| 2011 |
Faisal A, Vaughan L, Bavetsias V, Sun C, Atrash B, Avery S, Jamin Y, Robinson SP, Workman P, Blagg J, Raynaud FI, Eccles SA, Chesler L, Linardopoulos S. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Molecular Cancer Therapeutics. 10: 2115-23. PMID 21885865 DOI: 10.1158/1535-7163.Mct-11-0333 |
0.408 |
|
| 2011 |
Langdon SR, Brown N, Blagg J. Scaffold diversity of exemplified medicinal chemistry space. Journal of Chemical Information and Modeling. 51: 2174-85. PMID 21877753 DOI: 10.1021/Ci2001428 |
0.323 |
|
| 2011 |
Barillari C, Duncan AL, Westwood IM, Blagg J, van Montfort RL. Analysis of water patterns in protein kinase binding sites. Proteins. 79: 2109-21. PMID 21557316 DOI: 10.1002/Prot.23032 |
0.335 |
|
| 2011 |
Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, et al. Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorganic & Medicinal Chemistry Letters. 21: 2715-20. PMID 21195614 DOI: 10.1016/J.Bmcl.2010.11.120 |
0.446 |
|
| 2011 |
Moore AS, Faisal A, Bavetsias V, Castro DGd, Sun C, Atrash B, Valenti M, Brandon AdH, Avery S, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S. Resistance to Selective FLT3 Inhibitors, Driven by FLT3 Ligand and FLT3 Point Mutations, Can Be Overcome with the Dual FLT3-Aurora Kinase Inhibitor CCT241736, Blood. 118: 3492-3492. DOI: 10.1182/Blood.V118.21.3492.3492 |
0.346 |
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| 2011 |
Moore AS, Faisal A, Bavetsias V, Sun C, Atrash B, Valenti M, Brandon AdH, Avery S, Castro DGd, Raynaud FI, Workman P, Pearson AD, Blagg J, Eccles SA, Linardopoulos S. Abstract 3554: CCT137690, a dual inhibitor of Aurora and FLT3 kinases, sensitizes FLT3-ITD positive acute myeloid leukemia and overcomes resistance to selective FLT3-inhibition Cancer Research. 71: 3554-3554. DOI: 10.1158/1538-7445.Am2011-3554 |
0.411 |
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| 2011 |
Moore A, Faisal A, Bavetsias V, Castro DGd, Sun C, Atrash B, Valenti M, Brandon AdH, Avery S, Pearson A, Workman P, Blagg J, Raynaud F, Eccles S, Linardopoulos S. Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia. Molecular Cancer Therapeutics. 10. DOI: 10.1158/1535-7163.Targ-11-B74 |
0.384 |
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| 2010 |
Oberoi J, Richards MW, Crumpler S, Brown N, Blagg J, Bayliss R. Structural basis of poly(ADP-ribose) recognition by the multizinc binding domain of checkpoint with forkhead-associated and RING Domains (CHFR). The Journal of Biological Chemistry. 285: 39348-58. PMID 20880844 DOI: 10.1074/Jbc.M110.159855 |
0.307 |
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| 2010 |
Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V. Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells Bioorganic and Medicinal Chemistry Letters. 20: 5988-5993. PMID 20833547 DOI: 10.1016/J.Bmcl.2010.08.091 |
0.435 |
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| 2010 |
Ewan K, Pajak B, Stubbs M, Todd H, Barbeau O, Quevedo C, Botfield H, Young R, Ruddle R, Samuel L, Battersby A, Raynaud F, Allen N, Wilson S, Latinkic B, ... ... Blagg J, et al. A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Research. 70: 5963-73. PMID 20610623 DOI: 10.1158/0008-5472.Can-10-1028 |
0.356 |
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| 2010 |
Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, De Haven Brandon A, Box G, ... ... Blagg J, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of aurora kinases: Lead optimization studies toward the identification of an orally bioavailable preclinical development candidate Journal of Medicinal Chemistry. 53: 5213-5228. PMID 20565112 DOI: 10.1021/Jm100262J |
0.403 |
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| 2010 |
Lansdell MI, Hepworth D, Calabrese A, Brown AD, Blagg J, Burring DJ, Wilson P, Fradet D, Brown TB, Quinton F, Mistry N, Tang K, Mount N, Stacey P, Edmunds N, et al. Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. Journal of Medicinal Chemistry. 53: 3183-97. PMID 20329799 DOI: 10.1021/Jm9017866 |
0.309 |
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| 2010 |
Moore AS, Blagg J, Linardopoulos S, Pearson AD. Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias. Leukemia. 24: 671-8. PMID 20147976 DOI: 10.1038/Leu.2010.15 |
0.38 |
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| 2010 |
Dodson CA, Kosmopoulou M, Richards MW, Atrash B, Bavetsias V, Blagg J, Bayliss R. Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design. The Biochemical Journal. 427: 19-28. PMID 20067443 DOI: 10.1042/Bj20091530 |
0.389 |
|
| 2010 |
Moore AS, Faisal A, Bavetsias V, Sun C, Atrash B, Valenti M, Brandon AdH, Avery S, Raynaud FI, Workman P, Pearson AD, Blagg J, Eccles SA, Linardopoulos S. Dual Inhibition of Aurora and FLT3 Kinases by CCT137690: A Novel Treatment Strategy Against FLT3-ITD Positive AML In Vitro and In Vivo Blood. 116: 3289-3289. DOI: 10.1182/Blood.V116.21.3289.3289 |
0.364 |
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| 2010 |
Moore A, Bavetsias V, Sun C, Faisal A, Workman P, Blagg J, Pearson A, Linardopoulos S. Abstract 4428: A novel imidazo[4,5-b]pyridine Aurora kinase inhibitor with anti-leukemic activity Cancer Research. 70: 4428-4428. DOI: 10.1158/1538-7445.Am10-4428 |
0.374 |
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| 2009 |
Andrews MD, Green MP, Allerton CM, Batchelor DV, Blagg J, Brown AD, Gordon DW, McMurray G, Millns DJ, Nichols CL, Watson L. Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists. Bioorganic & Medicinal Chemistry Letters. 19: 5346-50. PMID 19692241 DOI: 10.1016/J.Bmcl.2009.07.133 |
0.35 |
|
| 2009 |
Rawjee T, Rowlands M, McAndrew C, Stubbs M, Lord CJ, Reis‐Filho JS, Ashworth A, Aherne W, Workman P, Blagg J, Linardopoulos S. Abstract A239: MPS1 (TTK) kinase inhibition selectively kills aneuploid cells Molecular Cancer Therapeutics. 8. DOI: 10.1158/1535-7163.Targ-09-A239 |
0.367 |
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| 2009 |
Kosmopoulou M, Faisal A, Sun C, Bavetsias V, Atrash B, Bouloc N, Matteucci M, Blagg J, Linardopoulos S, Bayliss R. How to design aurora kinase A selective inhibitors Acta Crystallographica Section A. 65: 148-149. DOI: 10.1107/S0108767309097013 |
0.354 |
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| 2007 |
Bunnage ME, Blagg J, Steele J, Owen DR, Allerton C, McElroy AB, Miller D, Ringer T, Butcher K, Beaumont K, Evans K, Gray AJ, Holland SJ, Feeder N, Moore RS, et al. Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. Journal of Medicinal Chemistry. 50: 6095-103. PMID 17990866 DOI: 10.1021/Jm0702433 |
0.405 |
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| 2007 |
Blagg J, Allerton CM, Batchelor DV, Baxter AD, Burring DJ, Carr CL, Cook AS, Nichols CL, Phipps J, Sanderson VG, Verrier H, Wong S. Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. Bioorganic & Medicinal Chemistry Letters. 17: 6691-6. PMID 17976986 DOI: 10.1016/J.Bmcl.2007.10.059 |
0.326 |
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| 2007 |
Fish PV, Allan GA, Bailey S, Blagg J, Butt R, Collis MG, Greiling D, James K, Kendall J, McElroy A, McCleverty D, Reed C, Webster R, Whitlock GA. Potent and selective nonpeptidic inhibitors of procollagen C-proteinase. Journal of Medicinal Chemistry. 50: 3442-56. PMID 17591762 DOI: 10.1021/Jm061010Z |
0.358 |
|
| 1996 |
Blagg J, Ballard SA, Cooper K, Finn PW, Johnson PS, MacIntyre F, Maw GN, Spargo PL. The development of non-steroidal dual inhibitors of both human 5α-reductase isozymes Bioorganic & Medicinal Chemistry Letters. 6: 1517-1522. DOI: 10.1016/S0960-894X(96)00261-2 |
0.37 |
|
| 1995 |
Harris MCJ, Whitby RJ, Blagg J. Convergent synthesis of pyrrolidines, piperidines, perhydroazepines and tetrahydroisoquinolines via zirconocene η2-imine complexes Tetrahedron Letters. 36: 4287-4290. DOI: 10.1016/0040-4039(95)00741-T |
0.303 |
|
| 1990 |
Oppolzer W, Blagg J, Rodriguez I, Walther E. Bornanesultam-directed asymmetric synthesis of crystalline, enantiomerically pure syn aldols Journal of the American Chemical Society. 112: 2767-2772. DOI: 10.1021/Ja00163A045 |
0.48 |
|
| 1990 |
Oppolzer W, Wills M, Kelly MJ, Signer M, Blagg J. Chiral toluene-2,α-sultam auxiliaries: Asymmetric diels-alder reactions of N-enoyl derivatives Tetrahedron Letters. 31: 5015-5018. DOI: 10.1016/S0040-4039(00)97793-1 |
0.506 |
|
| 1990 |
BLAGG J, DAVIES SG, GOODFELLOW CL, SUTTON KH. ChemInform Abstract: Regioselective Nucleophilic Additions to Tricarbonyl(η6-arene)chromium(0) Complexes: Electronic versus Chelation Control. Cheminform. 21. DOI: 10.1002/chin.199028236 |
0.335 |
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| 1989 |
Oppolzer W, Rodriguez I, Blagg J, Bernardinelli G. Asymmetric Diels‐Alder reactions: X‐Ray crystal‐structure analysis of [N‐((E)‐But‐2‐enoyl)bornane‐10,2‐sultam]tetrachlorotitanium Helvetica Chimica Acta. 72: 123-130. DOI: 10.1002/Hlca.19890720116 |
0.47 |
|
| 1988 |
BAIRD PD, BLAGG J, DAVIES SG, SUTTON KH. ChemInform Abstract: Stereospecific Synthesis of (-)-(8R) and (-)-(8S)-Methylcanadine Cheminform. 19. DOI: 10.1002/chin.198815354 |
0.332 |
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| 1988 |
BLAGG J, DAVIES SG. ChemInform Abstract: The Highly Stereoselective Conversion of N,N-Dimethylamphetamine into N-Methylpseudoephedrine; a Mimic of the Enzyme Mediated Stereospecific Benzylic Hydroxylation of 2-Arylethylamines. Cheminform. 19. DOI: 10.1002/chin.198809153 |
0.365 |
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| 1987 |
Blagg J, Davies SG. The highly stereoselective conversion of n,n-dimethylamphetamine into n-methylpseudoephedrine; A mimic of the enzyme mediated stereospecific benzylic h Tetrahedron. 43: 4463-4471. DOI: 10.1016/S0040-4020(01)90323-0 |
0.444 |
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| 1987 |
BLAGG J, DAVIES SG, GOODFELLOW CL, SUTTON KH. ChemInform Abstract: The Diastereoselective Functionalization of Arene Tricarbonylchromium Complexes Containing a Benzylic Heteroatom Substituent. Cheminform. 18. DOI: 10.1002/chin.198748270 |
0.364 |
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| 1987 |
BLAGG J, COOTE SJ, DAVIES SG, MIDDLEMISS D, NAYLOR A. ChemInform Abstract: Tetrahydroisoquinolines. Part 3. Stereoselective Synthesis of cis- and trans-1,4-Disubstituted N-Methyl-1,2,3,4-tetrahydroisoquinolines as Their Tricarbonylchromium Complexes. Cheminform. 18. DOI: 10.1002/chin.198729257 |
0.378 |
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| 1987 |
BLAGG J, COOTE SJ, DAVIES SG, MOBBS BE. ChemInform Abstract: Tetrahydroisoquinolines. Part 2. Synthesis of 4-Substituted N-Methyl-1,2,3,4-tetrahydroisoquinolines via Regio- and Stereo-Selective Elaboration of Tricarbonyl(N-methyl-1,2,3,4-tetrahydroisoquinoline)chromium. Cheminform. 18. DOI: 10.1002/chin.198718207 |
0.406 |
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| 1987 |
BLAGG J, DAVIES SG, HOLMAN NJ, LAUGHTON CA, MOBBS BE. ChemInform Abstract: Elaboration of α-Substituted Benzyl Alkyl Ethers and Sulfides by Suppression of the Wittig and Related Rearrangements via Complexation to Tricarbonylchromium. Cheminform. 18. DOI: 10.1002/chin.198704127 |
0.373 |
|
| 1986 |
Blagg J, Coote SJ, Davies SG, Mobbs BE. Tetrahydroisoquinolines. Part 2. Synthesis of 4-substituted N-methyl-1,2,3,4-tetrahydroisoquinolines via regio- and stereo-selective elaboration of tricarbonyl(N-methyl-1,2,3,4-tetrahydroisoqumoline)chromium Journal of the Chemical Society-Perkin Transactions 1. 2257-2261. DOI: 10.1039/P19860002257 |
0.328 |
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| 1986 |
Blagg J, Davies SG. The stereoselective synthesis of (–)-(8R)-methylcanadine via selective monocomplexation of canadine to chromium tricarbonyl Journal of the Chemical Society, Chemical Communications. 492-493. DOI: 10.1039/C39860000492 |
0.31 |
|
| 1986 |
BLAGG J, DAVIES SG. ChemInform Abstract: The Stereoselective Synthesis of (-)-(8R)-Methylcanadine via Selective Monocomplexation of Canadine to Chromium Tricarbonyl. Chemischer Informationsdienst. 17. DOI: 10.1002/Chin.198633303 |
0.443 |
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| 1985 |
Blagg J, Davies SG, Mobbs BE. 4-Substituted N-methyl-1,2,3,4-tetrahydroisoquinolines: synthesis via stereoselective substitution of tricarbonyl(N-methyl-1,2,3,4-tetrahydroisoquinoline)chromium Journal of the Chemical Society, Chemical Communications. 619-620. DOI: 10.1039/C39850000619 |
0.312 |
|
| 1985 |
BLAGG J, DAVIES SG. ChemInform Abstract: STEREOSPECIFIC CONVERSION OF N,N-DIMETHYLAMPHETAMINE INTO N-METHYLPSEUDOEPHEDRINE Chemischer Informationsdienst. 16. DOI: 10.1002/Chin.198536084 |
0.422 |
|
| 1985 |
BLAGG J, DAVIES SG, MOBBS BE. ChemInform Abstract: 4-SUBSTITUTED N-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINES: SYNTHESIS VIA STEREOSELECTIVE SUBSTITUTION OF TRICARBONYL(N-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINE)CHROMIUM Chemischer Informationsdienst. 16. DOI: 10.1002/Chin.198533245 |
0.469 |
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