publications

our publications.


Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Johnstone S; Albert JS. Bioorg. Med. Chem. Lett. 2017, 2239.

Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors. Varnes JG; Geschwindner S; Holmquist CR; Forst J; Wang X; Dekker N; Scott CW; Tian G; Wood MW; Albert JS. Bioorg. Med. Chem. Lett. 2016; 197.

Bromodomain inhibitors regulate the C9ORF72 locus in ALS. Zeier Z; Esanov R; Belle KC; Volmar C-H; Johnstone AL; Halley P; DeRosa BA; Khoury N; van Blitterswijk M; Rademakers R; Albert J; Brothers SP; Wuu J; Dykxhoorn DM; Benatar M; Wahlestedt C. Exp. Neurol. 2015; 241.

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists. Laliberte S; Vallee F; Fournier P-A; Bedard L; Labrecque J; Albert JS. Bioorg. Med. Chem. Lett. 2014; 3204.

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists. Hu, YJ; St.-Onge, M; Laliberte, S; Vallee, F, Jin, S; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3199.

Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists. Laliberte, S; Vallee, F; Fournier, PA; Bedard, L; Labrecque, J; Albert, JS. Biorg. Med. Chem. Lett., 2014, 24, 3204.

Development of a Plate-Based Optical Biosensor Fragment Screening Methodology to Identify Phosphodiesterase 10A Inhibitors. Geschwindner S, Dekker N, Horsefield R, Tigerstrom A, Johansson P, Scott CW, Albert JS, J. Med. Chem., 2013.

Multiple Roles of Transient Receptor Potential (TRP) Channels in Inflammatory Conditions and Current Status of Drug Development, Radresa, O,Paré, M, Albert, JS, 2013, Current Topics in Med. Chem., 2013.

Targets and Emerging Therapies for Schizophrenia, 2012, Wiley Publications, Editors: Albert, JS, Wood, MW.

Progress in the Exploration and Development of GlyT1 Inhibitors for Schizophrenia, Albert, JS, Wood, MW., 2012.

Isoquinucline-based GlyT1 inhibitors for schizophrenia: Discovery, optimization, synthesis, and in vivo pharmacology Albert, JS; ACS National Symposium, 2012.

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists, Brown, W, Johnstone, S, Jones, P, Walpole, C, Griffin, AW, et al. BMCL, 2012, 22, 6205.

N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration, Zhongyong W; Tremblay, M; Johnstone, S; Tomaszewski, M; Brown, W; Walpole, C; Page, D; et al. BMCL, 2012, 22, 3884.

Fragment-based lead discovery, Albert, JS, 2010, Wiley Publications.

Discovery of new high-affinity PDE10 inhibitors using fragment based lead generation and knowledge-based design, Albert, JS; ACS National Symposium, 2012.

Identification of high-affinity β-secretase inhibitors using fragment-based lead generation, Albert, JS, Edwards, PD, 2008.

An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca’s drug discovery programmes, Albert, JS; Blomberg, N., et al.

Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta -secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency, Edwards, PD; Albert, JS; et al.J. Med. Chem. 2007, 50, 5912-5925.

Neurokinin-3 receptor antagonists in schizophrenia, Albert, JS, Potts, W., Expert Opin.Ther. Pat. 2006, 16, 925-937.

our book.


Progress in the exploration and development of GlyT1 inhibitors for schizophrenia, Albert JS; Wood MW. John Wiley & Sons, Inc.; 2012.

our patents.


Preparation of substituted imidazopyridines as bromodomain inhibitors. Pourashraf, Mehrnaz; Beaulieu, Marc-Andre; Claridge, Stephen; Bayrakdarian, Malken; Johnstone, Shawn; Albert, Jeffrey S.; Griffin, Andrew; 2017. WO2017066876.

Substituted benzimidazoles as bromodomain inhibitors, their preparation and their use as pharmaceuticals. Pourashraf M; Jacquemot G; Claridge S; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017. WO2017024412.

N-Substituted bicyclic lactams as bromodomain inhibitors, their preparation and their use as pharmaceuticals. Jacquemot G; Claridge S; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017. WO2017024406.

Preparation of aryl-substituted dihydroquinolinones as bromodomain inhibitors. acquemot G; Bayrakdarian M; Johnstone S; Albert JS; Griffin A; 2017. WO2017024408.

Preparation of oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors. Albert JS; Johnstone S; Jones P; 2014. WO2014152029.

recent presentations.


Progress in strategies to optimize allosteric modulators. Johnstone S. Cambridge Healthtech Symposium, San Diego 2017.

Identification of inhibitors of HIF2a as modulators of the hypoxia response for the treatment of cancer. Johnstone S; Masek B; Wang L; Brothers S; Bourgault S; Grazinni E; Coupal M. ACS National Meeting 2016.

Development of highly potent, selective BET bromodomain inhibitors that are CNS penetrant and effective in rodent models of brain cancer. Bayrakdarian M; Johnstone A; Penas C; Stathias V; Brothers S; Ayad N; Wahlestedt C. ACS National Meeting 2016.