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Primary tabs

1. Personal Information

Jonathan Baell
My web page
WEHI, Note: This will change to MIPS in April 2012

2. Community Expertise

Malaria research
Schistosomiasis research
Chagas Research Community
Toxoplasma Research Community
Tuberculosis research community
The Synaptic Leap community

3. Publications


Since 2006:
24. Harvey AJ, Baell JB, Toovey NT, Homerick D & Wulff H. A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone. J. Med. Chem. 49, 1433-1441 (2006).
25. Baell JB, Duggan PJ, Forsyth SA, Lewis RJ, Lok YP, Schroeder CI & Shepherd NE. Synthesis and Biological Evaluation of Anthranilamide-Based Non-Peptide Mimetics of omega-conotoxin GIVA. Tetrahedron 62, 7284-7292 (2006).
26. Hirokawa Y, Levitzki A, Lessene G, Baell J & Maruta H. Signal Therapy of Human Pancreatic Cancer and NF1-deficient Multidrug-resistant Breast Cancer Xenograft in Mice by a Combination of PP1 and GL-2003, Anti-PAK1 Drugs (Tyr-kinase Inhibitors). Cancer Lett. 245, 242-51 (2007).
27. Nguyen TV, Matsuyama H, Baell J, Hunne B, Fowler CJ, Smith JE, Nurgali K, Furness JB. Effects of compounds that influence IK (KCNN4 channels) on after-hyperpolarizing potentials, and determination of IK channel sequence, in guinea pig enteric neurons. J. Neurophysiol. 97, 2024-2031 (2007).
28. Holloway GA, Baell JB, Fairlamb AH, Novello PM, Parisot JP, Richardson J, Watson KG & Street IP. Discovery of 2-iminobenzimidazoles as a new class of Trypanothione Reductase inhibitor by high throughput screening. Bioorg. Med. Chem. Lett. 17, 1422-1427 (2007).
29. Rye CS, Baell JB, Street IP. Synthesis, reactivity and applications of 1-fluoroalkyl carboxylates: novel synthetic substrates for esterases and lipases. Tetrahedron 63, 3306-3311 (2007).
30. Ferens D, Baell J, Lessene G, Smith E & Furness JB. Effects of modulators of Ca2+-activated, intermediate conductance potassium channels on motility of the rat small intestine, in vivo. Neurogastroenterol. Motil. 19, 383-389 (2007).
31. Cianci J, Baell JB & Harvey AJ. Microwave-assisted, zinc-mediated peptide coupling of N-benzyl-α, α -disubstituted amino acids. Tetrahedron Lett. 48, 5973-5975 (2007).
32. Cianci J, Baell JB, Flynn BL, Gable RW, Mould JA, Paul D & Harvey AJ. Synthesis and biological evaluation of chalcones as inhibitors of the voltage-gated potassium channel Kv1.3 Bioorg. Med. Chem. Lett. 18, 2055-2061 (2008).
33. Pietersz GA, Mottram PL, van de Velde NC, Sardjono CT, Esparon S, Ramsland PA, Moloney G, Baell JB, McCarthy TD, Matthews BR, Powell MS & Hogarth PM. Inhibition of destructive autoimmune arthritis in FcgRIIA transgenic mice by small chemical entities. Immunol. Cell Biol. 87, 3-12 (2009).
34. Holloway GA, Charman WN, Fairlamb AH, Brun R, Kaiser, M Kostewicz E, Novello PM, Parisot JP, Richardson J, Street IP, Watson KG & Baell, JB. Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with anti-parasitic activity. Antimicrob. Agents Chemother. 53, 2824-2833 (2009).
35. Lessene G, Smith BJ, Gable RW & Baell JB. Characterization of the two fundamental conformations of benzoylureas and elucidation of the factors that facilitate their conformational interchange. J. Org. Chem. 74 , 6511-6525 (2009).
36. Andersson A, Baell JB, Duggan PJ, Graham JE, Lewis RJ, Lumsden NG, Tranberg CE, Tuck KL & Yang A. w-Conotoxin GVIA mimetics based on an anthranilamide core: effect of variation in ammonium side chain lengths and incorporation of fluorine. Bioorg. Med. Chem. 17, 6659-6670 (2009).
37. Baell JB & Holloway GA. New substructure filters for removal of pan assay interference compounds [PAINS] from screening libraries and for their exclusion in bioassays. J. Med. Chem. 53, 2719-2740 (2010).
38. Sleebs BE, Street IP, Bu X & Baell JB. De novo synthesis of a potent LIMK1 inhibitor. Synthesis 7, 1091-1096 (2010).
39. Holloway GA, Parisot JP, Novello PM, Watson KG, Armstrong T, Thompson RCA, Street IP & Baell JB. Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi. Bioorg. Med. Chem. Lett. 20, 1816-1818 (2010).
40. Lackovic K, Parisot JP, Sleebs N, Baell JB, Debien L, Watson KG, Curtis JM, Handman E, Street IP & Kedzierski L. Inhibitors of Leishmania GDP-Mannose Pyrophosphorylase Identified by High-Throughput Screening of Small Molecule Chemical Library. Antimicrob. Agents Chemother. 54, 1712-1719 (2010).
41. Nhu D, Duffy S, Avery VM, Hughes AH & Baell JB. 3-Arylamino-6-benzylamino-1,2,4,5-tetrazines with potent antimalarial activity. Bioorg. Med. Chem. Lett. 20, 4496-4498 (2010)
42. Ban K, Duffy S, Khakham Y, Avery VM, Hughes AH, Montagnat O, Katneni K, Ryan E & Baell JB. 3-Alkylthio-1,2,4-triazine dimers with potent antimalarial activity. Bioorg. Med. Chem. Lett. 20, 6024-6029 (2010).
43. Baell JB. Observations on Screening-Based Research and Some Concerning Trends in the Literature. Future Med. Chem. 2, 1529–1546 (2010).
44. Brady RM, Khakham Y, Lessene G & Baell JB. Benzoylureas as removable cis amide inducers: synthesis of cyclic amides via ring closing metathesis (RCM). Org. Biomol. Chem. 9, 656-658 (2011).
45. Sleebs BE, Czabotar PE, Fairbrother, WJ, Fairlie WD, Flygare, JA, Huang, DCS, Kersten WJA, Koehler MFT, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H & Baell, JB. Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 (Bcl-2) and B-cell lymphoma extra long (Bcl-xL) with potent pro-apoptotic cell-based activity. J. Med. Chem. 54, 1914-1926 (2011).
46. Lagorce D, Maupetit J, Baell J, Sperandio O, Tuffery P, Miteva MA, Galons H, Villoutreix BO. The FAF-Drugs2 server: a multistep engine to prepare electronic compound collections. Bioinformatics 27, 2018-2020 (2011).
47. Saubern S, Guha R, Baell JB. KNIME workflow to assess PAINS filters in SMARTS format. Comparison of RDKit and Indigo cheminformatics libraries. Mol. Informatics DOI : 10.1002/minf.201100076.
48. Sleebs BE, Nikolakopoulos G, Street IP, Falk H, Baell JB. Identification of 5,6-substituted4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors. Bioorg. Med. Chem. Lett. 21, 5992-5994 (2011).
49. Sleebs BE, Levit A, Street IP, Falk H, Hammonds T, Wong AC, Charles MD, Olson MF, Baell JB. Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors. Med. Chem. Commun. 2, 977-981 (2011).
50. Sleebs BE, Ganame D, Levit A, Street IP, Gregg A, Falk H, Baell JB. Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors. Med. Chem. Commun. 2, 982-986 (2011).
51. Falk H, Connor T, Yang H, Loft KJ, Alcindor JL, Nikolakopoulos GE, Surjadi RN, Bentley JD, Hattarki MK, Dolezal O, Murphy JM, Monohan BJ, Peat TS, Thomas T, Baell JB, Parisot JP, Street IP. An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets. J. Biomol. Screening 16, 1196-1205 (2011).
52. Baell JB. Redox active nuisance screening compounds and their classification. Drug Discov. Today 16, 840-841 (2011).
53. Taboureau O, Baell JB, Recio J-F, Villoutreix BO. Established and emerging trends in computational drug discovery in the structural genomics era. Chemistry & Biology 19. 29-41 (2012).
54. Sykes ML, Baell JB, Kaiser M, Chatelain E, Ganame D, Ioset J, Avery VM. Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei BS427 by a whole cell viability based HTS campaign . Plos Neglected Tropical Diseases (accepted).
55. Li R, Doherty J, Antonipillai J, Chen S, Devlin M, Visser K, Baell J, Street I, Anderson RL, Bernard O. LIM kinase inhibition reduces breast cancer growth and invasiveness but not metastasis in mice. Clinical Cancer Research (submitted).


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