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Stockholm, Sweden

Larsson A.,Nanyang Technological University | Jansson A.,Nanyang Technological University | Aberg A.,Karolinska Institutet | Aberg A.,Sprint Bioscience | And 2 more authors.
Current Opinion in Chemical Biology | Year: 2011

Fragment-based ligand discovery constitutes a useful strategy for the generation of high affinity ligands with suitable physico-chemical properties to serve as drug leads. There is an increasing number of generic biophysical screening strategies established with the potential for accelerating the generation of useful fragment hits. Crystal structures of these hits can subsequently be used as starting points for fragment evolution to high affinity ligands. Emerging understanding of the efficiency and operative aspects of hit generation and structural characterization in FBLD suggests that this method should be well suited for academic ligand development of chemical tools and experimental therapeutics. © 2011 Elsevier Ltd. Source


Viklund J.,Astrazeneca | Kolmodin K.,Astrazeneca | Nordvall G.,Astrazeneca | Swahn B.-M.,Astrazeneca | And 4 more authors.
ACS Medicinal Chemistry Letters | Year: 2014

In order to find optimal core structures as starting points for lead optimization, a multiparameter lead generation workflow was designed with the goal of finding BACE-1 inhibitors as a treatment for Alzheimer's disease. De novo design of core fragments was connected with three predictive in silico models addressing target affinity, permeability, and hERG activity, in order to guide synthesis. Taking advantage of an additive SAR, the prioritized cores were decorated with a few, well-characterized substituents from known BACE-1 inhibitors in order to allow for core-to-core comparisons. Prediction methods and analyses of how physicochemical properties of the core structures correlate to in vitro data are described. The syntheses and in vitro data of the test compounds are reported in a separate paper by Ginman et al. [J. Med. Chem. 2013, 56, 4181-4205]. The affinity predictions are described in detail by Roos et al. [J. Chem. Inf. 2014, DOI: 10.1021/ci400374z]. © 2014 American Chemical Society. Source


Sprint Bioscience | Entity website

Visiting address Novum Hlsovgen 7, 8th floor Huddinge Postal address Novum 141 57 Huddinge Sweden Telephone +46 (0)8-411 44 55


Sprint Bioscience | Entity website

Visiting address Novum Hlsovgen 7, 8th floor Huddinge Postal address Novum 141 57 Huddinge Sweden Telephone +46 (0)8-411 44 55


Sprint Bioscience | Entity website

Calendar 7 November, 2016 I the beginning of November, BIO Europe is held, and this time in Cologne, Germany. SprintBioscience will participate to meet with representatives from our global network and to establish new contacts, as the meeting is Europes largest Investand Partnering meeting ...

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