1.

Romasanta, A. K. S.; van der Sijde, P.; Hellsten, I.; Hubbard, R. E.; Keseru, G. M.; van Muijlwijk-Koezen, J.; de Esch, I. J. P. When fragments link: a bibliometric perspective on the development of fragment-based drug discovery. Drug Discov Today 2018.

2.

Rachman, M. M.; Barril, X.; Hubbard, R. E. Predicting how drug molecules bind to their protein targets. Curr Opin Pharmacol 2018, 42, 34-39.

3.

Massey, A. J. A high content, high throughput cellular thermal stability assay for measuring drug-target engagement in living cells. PLoS One 2018, 13, e0195050.

4.

Lamoree, B.; Hubbard, R. E. Using Fragment-Based Approaches to Discover New Antibiotics. SLAS Discov 2018, 23, 495-510.

5.

Geneste, C. C.; Massey, A. J. Cell Density Affects the Detection of Chk1 Target Engagement by the Selective Inhibitor V158411. SLAS Discov 2018, 23, 144-153.

6.

Casara, P.; Davidson, J.; Claperon, A.; Le Toumelin-Braizat, G.; Vogler, M.; Bruno, A.; Chanrion, M.; Lysiak-Auvity, G.; Le Diguarher, T.; Starck, J. B.; Chen, I.; Whitehead, N.; Graham, C.; Matassova, N.; Dokurno, P.; Pedder, C.; Wang, Y.; Qiu, S.; Girard, A. M.; Schneider, E.; Grave, F.; Studeny, A.; Guasconi, G.; Rocchetti, F.; Maiga, S.; Henlin, J. M.; Colland, F.; Kraus-Berthier, L.; Le Gouill, S.; Dyer, M. J. S.; Hubbard, R.; Wood, M.; Amiot, M.; Cohen, G. M.; Hickman, J. A.; Morris, E.; Murray, J.; Geneste, O. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget 2018, 9, 20075-20088.

7.

Williamson, D. S.; Smith, G. P.; Acheson-Dossang, P.; Bedford, S. T.; Chell, V.; Chen, I. J.; Daechsel, J. C. A.; Daniels, Z.; David, L.; Dokurno, P.; Hentzer, M.; Herzig, M. C.; Hubbard, R. E.; Moore, J. D.; Murray, J. B.; Newland, S.; Ray, S. C.; Shaw, T.; Surgenor, A. E.; Terry, L.; Thirstrup, K.; Wang, Y.; Christensen, K. V. Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1). J Med Chem 2017, 60, 8945-8962.

8.

Thirstrup, K.; Dachsel, J. C.; Oppermann, F. S.; Williamson, D. S.; Smith, G. P.; Fog, K.; Christensen, K. V. Selective LRRK2 kinase inhibition reduces phosphorylation of endogenous Rab10 and Rab12 in human peripheral mononuclear blood cells. Sci Rep 2017, 7, 10300.

9.

Smith, G. P.; Badolo, L.; Chell, V.; Chen, I. J.; Christensen, K. V.; David, L.; Daechsel, J. A.; Hentzer, M.; Herzig, M. C.; Mikkelsen, G. K.; Watson, S. P.; Williamson, D. S. The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors. Bioorg Med Chem Lett 2017, 27, 4500-4505.

10.

Ruiz-Carmona, S.; Schmidtke, P.; Luque, F. J.; Baker, L.; Matassova, N.; Davis, B.; Roughley, S.; Murray, J.; Hubbard, R.; Barril, X. Dynamic undocking and the quasi-bound state as tools for drug discovery. Nat Chem 2017, 9, 201-206.

11.

Massey, A. J. Modification of tumour cell metabolism modulates sensitivity to Chk1 inhibitor-induced DNA damage. Sci Rep 2017, 7, 40778.

12.

Lamoree, B.; Hubbard, R. E. Current perspectives in fragment-based lead discovery (FBLD). Essays Biochem 2017, 61, 453-464.

13.

Darby, J. F.; Atobe, M.; Firth, J. D.; Bond, P.; Davies, G. J.; O'Brien, P.; Hubbard, R. E. Increase of enzyme activity through specific covalent modification with fragments. Chem Sci 2017, 8, 7772-7779.

14.

Christensen, K. V.; Smith, G. P.; Williamson, D. S. Development of LRRK2 Inhibitors for the Treatment of Parkinson's Disease. Prog Med Chem 2017, 56, 37-80.

15.

Brough, P. A.; Baker, L.; Bedford, S.; Brown, K.; Chavda, S.; Chell, V.; D'Alessandro, J.; Davies, N. G.; Davis, B.; Le Strat, L.; Macias, A. T.; Maddox, D.; Mahon, P. C.; Massey, A. J.; Matassova, N.; McKenna, S.; Meissner, J. W.; Moore, J. D.; Murray, J. B.; Northfield, C. J.; Parry, C.; Parsons, R.; Roughley, S. D.; Shaw, T.; Simmonite, H.; Stokes, S.; Surgenor, A.; Stefaniak, E.; Robertson, A.; Wang, Y.; Webb, P.; Whitehead, N.; Wood, M. Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase. J Med Chem 2017, 60, 2271-2286.

16.

Wayne, J.; Brooks, T.; Massey, A. J. Inhibition of Chk1 with the small molecule inhibitor V158411 induces DNA damage and cell death in an unperturbed S-phase. Oncotarget 2016, 7, 85033-85048.

17.

Renaud, J. P.; Chung, C. W.; Danielson, U. H.; Egner, U.; Hennig, M.; Hubbard, R. E.; Nar, H. Biophysics in drug discovery: impact, challenges and opportunities. Nat Rev Drug Discov 2016, 15, 679-698.

18.

Pawsey, S.; Wood, M.; Browne, H.; Donaldson, K.; Christie, M.; Warrington, S. Safety, Tolerability and Pharmacokinetics of FAAH Inhibitor V158866: A Double-Blind, Randomised, Placebo-Controlled Phase I Study in Healthy Volunteers. Drugs R D 2016, 16, 181-191.

19.

Massey, A. J.; Stephens, P.; Rawlinson, R.; McGurk, L.; Plummer, R.; Curtin, N. J. mTORC1 and DNA-PKcs as novel molecular determinants of sensitivity to Chk1 inhibition. Mol Oncol 2016, 10, 101-112.

20.

Massey, A. J. Inhibition of ATR-dependent feedback activation of Chk1 sensitises cancer cells to Chk1 inhibitor monotherapy. Cancer Lett 2016, 383, 41-52.

21.

Massey, A. J. Tumour growth environment modulates Chk1 signalling pathways and Chk1 inhibitor sensitivity. Sci Rep 2016, 6, 35874.

22.

Kotschy, A.; Szlavik, Z.; Murray, J.; Davidson, J.; Maragno, A. L.; Le Toumelin-Braizat, G.; Chanrion, M.; Kelly, G. L.; Gong, J. N.; Moujalled, D. M.; Bruno, A.; Csekei, M.; Paczal, A.; Szabo, Z. B.; Sipos, S.; Radics, G.; Proszenyak, A.; Balint, B.; Ondi, L.; Blasko, G.; Robertson, A.; Surgenor, A.; Dokurno, P.; Chen, I.; Matassova, N.; Smith, J.; Pedder, C.; Graham, C.; Studeny, A.; Lysiak-Auvity, G.; Girard, A. M.; Grave, F.; Segal, D.; Riffkin, C. D.; Pomilio, G.; Galbraith, L. C.; Aubrey, B. J.; Brennan, M. S.; Herold, M. J.; Chang, C.; Guasconi, G.; Cauquil, N.; Melchiore, F.; Guigal-Stephan, N.; Lockhart, B.; Colland, F.; Hickman, J. A.; Roberts, A. W.; Huang, D. C.; Wei, A. H.; Strasser, A.; Lessene, G.; Geneste, O. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models. Nature 2016, 538, 477-482.

23.

Foloppe, N.; Chen, I. J. Towards understanding the unbound state of drug compounds: Implications for the intramolecular reorganization energy upon binding. Bioorg Med Chem 2016, 24, 2159-2189.

24.

Erlanson, D. A.; Fesik, S. W.; Hubbard, R. E.; Jahnke, W.; Jhoti, H. Twenty years on: the impact of fragments on drug discovery. Nat Rev Drug Discov 2016, 15, 605-619.

25.

Stocchi, F.; Vacca, L.; Grassini, P.; Pawsey, S.; Whale, H.; Marconi, S.; Torti, M. L-Dopa Pharmacokinetic Profile with Effervescent Melevodopa/Carbidopa versus Standard-Release Levodopa/Carbidopa Tablets in Parkinson's Disease: A Randomised Study. Parkinsons Dis 2015, 2015, 369465.

26.

Massey, A. J.; Stokes, S.; Browne, H.; Foloppe, N.; Fiumana, A.; Scrace, S.; Fallowfield, M.; Bedford, S.; Webb, P.; Baker, L.; Christie, M.; Drysdale, M. J.; Wood, M. Identification of novel, in vivo active Chk1 inhibitors utilizing structure guided drug design. Oncotarget 2015, 6, 35797-35812.

27.

Massey, A. J. Multiparametric Cell Cycle Analysis Using the Operetta High-Content Imager and Harmony Software with PhenoLOGIC. PLoS One 2015, 10, e0134306.

28.

Luthy, M.; Wheldon, M. C.; Haji-Cheteh, C.; Atobe, M.; Bond, P. S.; O'Brien, P.; Hubbard, R. E.; Fairlamb, I. J. Lead-oriented synthesis: Investigation of organolithium-mediated routes to 3-D scaffolds and 3-D shape analysis of a virtual lead-like library. Bioorg Med Chem 2015, 23, 2680-2694.

29.

Ruiz-Carmona, S.; Alvarez-Garcia, D.; Foloppe, N.; Garmendia-Doval, A. B.; Juhos, S.; Schmidtke, P.; Barril, X.; Hubbard, R. E.; Morley, S. D. rDock: a fast, versatile and open source program for docking ligands to proteins and nucleic acids. PLoS Comput Biol 2014, 10, e1003571.

30.

Rawlinson, R.; Massey, A. J. gammaH2AX and Chk1 phosphorylation as predictive pharmacodynamic biomarkers of Chk1 inhibitor-chemotherapy combination treatments. BMC Cancer 2014, 14, 483.

31.

Murray, J. B.; Roughley, S. D.; Matassova, N.; Brough, P. A. Off-rate screening (ORS) by surface plasmon resonance. An efficient method to kinetically sample hit to lead chemical space from unpurified reaction products. J Med Chem 2014, 57, 2845-2850.

32.

Moore, J. D.; Staniszewska, A.; Shaw, T.; D'Alessandro, J.; Davis, B.; Surgenor, A.; Baker, L.; Matassova, N.; Murray, J.; Macias, A.; Brough, P.; Wood, M.; Mahon, P. C. VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget 2014, 5, 12862-12876.

33.

Milner, S. J.; Snelling, A. M.; Kerr, K. G.; Abd-El-Aziz, A.; Thomas, G. H.; Hubbard, R. E.; Routledge, A.; Duhme-Klair, A. K. Probing linker design in citric acid-ciprofloxacin conjugates. Bioorg Med Chem 2014, 22, 4499-4505.

34.

Bryant, C.; Scriven, K.; Massey, A. J. Inhibition of the checkpoint kinase Chk1 induces DNA damage and cell death in human Leukemia and Lymphoma cells. Mol Cancer 2014, 13, 147.

35.

Bryant, C.; Rawlinson, R.; Massey, A. J. Chk1 inhibition as a novel therapeutic strategy for treating triple-negative breast and ovarian cancers. BMC Cancer 2014, 14, 570.

36.

Tabusa, H.; Brooks, T.; Massey, A. J. Knockdown of PAK4 or PAK1 inhibits the proliferation of mutant KRAS colon cancer cells independently of RAF/MEK/ERK and PI3K/AKT signaling. Mol Cancer Res 2013, 11, 109-121.

37.

Moore, J. D. In the wrong place at the wrong time: does cyclin mislocalization drive oncogenic transformation? Nat Rev Cancer 2013, 13, 201-208.

38.

Foloppe, N.; Gueroult, M.; Hartmann, B. Simulating DNA by molecular dynamics: aims, methods, and validation. Methods Mol Biol 2013, 924, 445-468.

39.

Davis, B. J.; Erlanson, D. A. Learning from our mistakes: the 'unknown knowns' in fragment screening. Bioorg Med Chem Lett 2013, 23, 2844-2852.

40.

Davis, B. Screening protein-small molecule interactions by NMR. Methods Mol Biol 2013, 1008, 389-413.

41.

Chen, I. J.; Foloppe, N. Tackling the conformational sampling of larger flexible compounds and macrocycles in pharmacology and drug discovery. Bioorg Med Chem 2013, 21, 7898-7920.

42.

Roughley, S. D.; Browne, H.; Macias, A. T.; Benwell, K.; Brooks, T.; D'Alessandro, J.; Daniels, Z.; Dugdale, S.; Francis, G.; Gibbons, B.; Hart, T.; Haymes, T.; Kennett, G.; Lightowler, S.; Matassova, N.; Mansell, H.; Merrett, A.; Misra, A.; Padfield, A.; Parsons, R.; Pratt, R.; Robertson, A.; Simmonite, H.; Tan, K.; Walls, S. B.; Wong, M. Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity. Bioorg Med Chem Lett 2012, 22, 901-906.

43.

Roughley, S.; Wright, L.; Brough, P.; Massey, A.; Hubbard, R. E. Hsp90 inhibitors and drugs from fragment and virtual screening. Top Curr Chem 2012, 317, 61-82.

44.

Davies, N. G.; Browne, H.; Davis, B.; Drysdale, M. J.; Foloppe, N.; Geoffrey, S.; Gibbons, B.; Hart, T.; Hubbard, R.; Jensen, M. R.; Mansell, H.; Massey, A.; Matassova, N.; Moore, J. D.; Murray, J.; Pratt, R.; Ray, S.; Robertson, A.; Roughley, S. D.; Schoepfer, J.; Scriven, K.; Simmonite, H.; Stokes, S.; Surgenor, A.; Webb, P.; Wood, M.; Wright, L.; Brough, P. Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization. Bioorg Med Chem 2012, 20, 6770-6789.

45.

Roughley, S. D.; Jordan, A. M. The medicinal chemist's toolbox: an analysis of reactions used in the pursuit of drug candidates. J Med Chem 2011, 54, 3451-3479.

46.

Roughley, S. D.; Hubbard, R. E. How well can fragments explore accessed chemical space? A case study from heat shock protein 90. J Med Chem 2011, 54, 3989-4005.

47.

Macias, A. T.; Williamson, D. S.; Allen, N.; Borgognoni, J.; Clay, A.; Daniels, Z.; Dokurno, P.; Drysdale, M. J.; Francis, G. L.; Graham, C. J.; Howes, R.; Matassova, N.; Murray, J. B.; Parsons, R.; Shaw, T.; Surgenor, A. E.; Terry, L.; Wang, Y.; Wood, M.; Massey, A. J. Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity. J Med Chem 2011, 54, 4034-4041.

48.

Hubbard, R. E.; Murray, J. B. Experiences in fragment-based lead discovery. Methods Enzymol 2011, 493, 509-531.

49.

Hubbard, R. E. Structure-based drug discovery and protein targets in the CNS. Neuropharmacology 2011, 60, 7-23.

50.

Foloppe, N. The benefits of constructing leads from fragment hits. Future Med Chem 2011, 3, 1111-1115.

51.

East, S. P.; Ayscough, A.; Toogood-Johnson, I.; Taylor, S.; Thomas, W. Peptidomimetic inhibitors of bacterial peptide deformylase. Bioorg Med Chem Lett 2011, 21, 4032-4035.

52.

Potter, A. J.; Ray, S.; Gueritz, L.; Nunns, C. L.; Bryant, C. J.; Scrace, S. F.; Matassova, N.; Baker, L.; Dokurno, P.; Robinson, D. A.; Surgenor, A. E.; Davis, B.; Murray, J. B.; Richardson, C. M.; Moore, J. D. Structure-guided design of alpha-amino acid-derived Pin1 inhibitors. Bioorg Med Chem Lett 2010, 20, 586-590.

53.

Potter, A.; Oldfield, V.; Nunns, C.; Fromont, C.; Ray, S.; Northfield, C. J.; Bryant, C. J.; Scrace, S. F.; Robinson, D.; Matossova, N.; Baker, L.; Dokurno, P.; Surgenor, A. E.; Davis, B.; Richardson, C. M.; Murray, J. B.; Moore, J. D. Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution. Bioorg Med Chem Lett 2010, 20, 6483-6488.

54.

Michel, J.; Foloppe, N.; Essex, J. W. Rigorous Free Energy Calculations in Structure-Based Drug Design. Mol Inform 2010, 29, 570-578.

55.

Massey, A. J.; Williamson, D. S.; Browne, H.; Murray, J. B.; Dokurno, P.; Shaw, T.; Macias, A. T.; Daniels, Z.; Geoffroy, S.; Dopson, M.; Lavan, P.; Matassova, N.; Francis, G. L.; Graham, C. J.; Parsons, R.; Wang, Y.; Padfield, A.; Comer, M.; Drysdale, M. J.; Wood, M. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol 2010, 66, 535-545.

56.

Massey, A. J.; Borgognoni, J.; Bentley, C.; Foloppe, N.; Fiumana, A.; Walmsley, L. Context-dependent cell cycle checkpoint abrogation by a novel kinase inhibitor. PLoS One 2010, 5, e13123.

57.

Massey, A. J. ATPases as drug targets: insights from heat shock proteins 70 and 90. J Med Chem 2010, 53, 7280-7286.

58.

Chen, I. J.; Foloppe, N. Drug-like bioactive structures and conformational coverage with the LigPrep/ConfGen suite: comparison to programs MOE and catalyst. J Chem Inf Model 2010, 50, 822-839.

59.

Williamson, D. S.; Borgognoni, J.; Clay, A.; Daniels, Z.; Dokurno, P.; Drysdale, M. J.; Foloppe, N.; Francis, G. L.; Graham, C. J.; Howes, R.; Macias, A. T.; Murray, J. B.; Parsons, R.; Shaw, T.; Surgenor, A. E.; Terry, L.; Wang, Y.; Wood, M.; Massey, A. J. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. J Med Chem 2009, 52, 1510-1513.

60.

Wade, A.; Pawsey, S.; Whale, H.; Boyce, M.; Warrington, S. Pharmacokinetics of two 6-day frovatriptan dosing regimens used for the short-term prevention of menstrual migraine: A phase I, randomized, double-blind, placebo-controlled, two-period crossover, single-centre study in healthy female volunteers. Clin Drug Investig 2009, 29, 325-337.

61.

Jordan, A. M.; Roughley, S. D. Drug discovery chemistry: a primer for the non-specialist. Drug Discov Today 2009, 14, 731-744.

62.

Hart, T.; Macias, A. T.; Benwell, K.; Brooks, T.; D'Alessandro, J.; Dokurno, P.; Francis, G.; Gibbons, B.; Haymes, T.; Kennett, G.; Lightowler, S.; Mansell, H.; Matassova, N.; Misra, A.; Padfield, A.; Parsons, R.; Pratt, R.; Robertson, A.; Walls, S.; Wong, M.; Roughley, S. Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. Bioorg Med Chem Lett 2009, 19, 4241-4244.

63.

Gillespie, R. J.; Bamford, S. J.; Gaur, S.; Jordan, A. M.; Lerpiniere, J.; Mansell, H. L.; Stratton, G. C. Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. Bioorg Med Chem Lett 2009, 19, 2664-2667.

64.

Gillespie, R. J.; Bamford, S. J.; Clay, A.; Gaur, S.; Haymes, T.; Jackson, P. S.; Jordan, A. M.; Klenke, B.; Leonardi, S.; Liu, J.; Mansell, H. L.; Ng, S.; Saadi, M.; Simmonite, H.; Stratton, G. C.; Todd, R. S.; Williamson, D. S.; Yule, I. A. Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides. Bioorg Med Chem 2009, 17, 6590-6605.

65.

Gillespie, R. J.; Bamford, S. J.; Botting, R.; Comer, M.; Denny, S.; Gaur, S.; Griffin, M.; Jordan, A. M.; Knight, A. R.; Lerpiniere, J.; Leonardi, S.; Lightowler, S.; McAteer, S.; Merrett, A.; Misra, A.; Padfield, A.; Reece, M.; Saadi, M.; Selwood, D. L.; Stratton, G. C.; Surry, D.; Todd, R.; Tong, X.; Ruston, V.; Upton, R.; Weiss, S. M. Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem 2009, 52, 33-47.

66.

Foloppe, N.; Chen, I. J. Conformational sampling and energetics of drug-like molecules. Curr Med Chem 2009, 16, 3381-3413.

67.

Foloppe, N.; Benwell, K.; Brooks, T. D.; Kennett, G.; Knight, A. R.; Misra, A.; Monck, N. J. Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. Bioorg Med Chem Lett 2009, 19, 4183-4190.

68.

Chen, I. J.; Hubbard, R. E. Lessons for fragment library design: analysis of output from multiple screening campaigns. J Comput Aided Mol Des 2009, 23, 603-620.

69.

Brough, P. A.; Barril, X.; Borgognoni, J.; Chene, P.; Davies, N. G.; Davis, B.; Drysdale, M. J.; Dymock, B.; Eccles, S. A.; Garcia-Echeverria, C.; Fromont, C.; Hayes, A.; Hubbard, R. E.; Jordan, A. M.; Jensen, M. R.; Massey, A.; Merrett, A.; Padfield, A.; Parsons, R.; Radimerski, T.; Raynaud, F. I.; Robertson, A.; Roughley, S. D.; Schoepfer, J.; Simmonite, H.; Sharp, S. Y.; Surgenor, A.; Valenti, M.; Walls, S.; Webb, P.; Wood, M.; Workman, P.; Wright, L. Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone. J Med Chem 2009, 52, 4794-4809.

70.

Bedford, S. T.; Benwell, K. R.; Brooks, T.; Chen, I.; Comer, M.; Dugdale, S.; Haymes, T.; Jordan, A. M.; Kennett, G. A.; Knight, A. R.; Klenke, B.; LeStrat, L.; Merrett, A.; Misra, A.; Lightowler, S.; Padfield, A.; Poullennec, K.; Reece, M.; Simmonite, H.; Wong, M.; Yule, I. A. Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor. Bioorg Med Chem Lett 2009, 19, 5945-5949.

71.

Scrace, S. F.; Kierstan, P.; Borgognoni, J.; Wang, L. Z.; Denny, S.; Wayne, J.; Bentley, C.; Cansfield, A. D.; Jackson, P. S.; Lockie, A. M.; Curtin, N. J.; Newell, D. R.; Williamson, D. S.; Moore, J. D. Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked. Cell Cycle 2008, 7, 3898-3907.

72.

Monck, N. J.; Kennett, G. A. 5-HT2C ligands: recent progress. Prog Med Chem 2008, 46, 281-390.

73.

Hubbard, R. E. Fragment approaches in structure-based drug discovery. J Synchrotron Radiat 2008, 15, 227-230.

74.

Gillespie, R. J.; Cliffe, I. A.; Dawson, C. E.; Dourish, C. T.; Gaur, S.; Jordan, A. M.; Knight, A. R.; Lerpiniere, J.; Misra, A.; Pratt, R. M.; Roffey, J.; Stratton, G. C.; Upton, R.; Weiss, S. M.; Williamson, D. S. Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines. Bioorg Med Chem Lett 2008, 18, 2924-2929.

75.

Gillespie, R. J.; Cliffe, I. A.; Dawson, C. E.; Dourish, C. T.; Gaur, S.; Giles, P. R.; Jordan, A. M.; Knight, A. R.; Lawrence, A.; Lerpiniere, J.; Misra, A.; Pratt, R. M.; Todd, R. S.; Upton, R.; Weiss, S. M.; Williamson, D. S. Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett 2008, 18, 2920-2923.

76.

Gillespie, R. J.; Adams, D. R.; Bebbington, D.; Benwell, K.; Cliffe, I. A.; Dawson, C. E.; Dourish, C. T.; Fletcher, A.; Gaur, S.; Giles, P. R.; Jordan, A. M.; Knight, A. R.; Knutsen, L. J.; Lawrence, A.; Lerpiniere, J.; Misra, A.; Porter, R. H.; Pratt, R. M.; Shepherd, R.; Upton, R.; Ward, S. E.; Weiss, S. M.; Williamson, D. S. Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett 2008, 18, 2916-2919.

77.

Foloppe, N.; Allen, N. H.; Bentley, C. H.; Brooks, T. D.; Kennett, G.; Knight, A. R.; Leonardi, S.; Misra, A.; Monck, N. J.; Sellwood, D. M. Discovery of a novel class of selective human CB1 inverse agonists. Bioorg Med Chem Lett 2008, 18, 1199-1206.

78.

Drysdale, M. J.; Brough, P. A. Medicinal chemistry of Hsp90 inhibitors. Curr Top Med Chem 2008, 8, 859-868.

79.

Chen, I. J.; Foloppe, N. Conformational sampling of druglike molecules with MOE and catalyst: implications for pharmacophore modeling and virtual screening. J Chem Inf Model 2008, 48, 1773-1791.

80.

Brough, P. A.; Aherne, W.; Barril, X.; Borgognoni, J.; Boxall, K.; Cansfield, J. E.; Cheung, K. M.; Collins, I.; Davies, N. G.; Drysdale, M. J.; Dymock, B.; Eccles, S. A.; Finch, H.; Fink, A.; Hayes, A.; Howes, R.; Hubbard, R. E.; James, K.; Jordan, A. M.; Lockie, A.; Martins, V.; Massey, A.; Matthews, T. P.; McDonald, E.; Northfield, C. J.; Pearl, L. H.; Prodromou, C.; Ray, S.; Raynaud, F. I.; Roughley, S. D.; Sharp, S. Y.; Surgenor, A.; Walmsley, D. L.; Webb, P.; Wood, M.; Workman, P.; Wright, L. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem 2008, 51, 196-218.