By Johan Schultz

iNovacia AB, Stockholm, Sweden, was created in 2006 as a scientist buy-out from Biovitrum, which in turn was a spin-out in 2001 from Pharmacia Corporation. iNovacia is now an established drug innovator providing discovery services to pharmaceutical and biotech companies in Europe and the US. We specialize in providing competitive preclinical candidates applying technologies to build a strong foundation for the understanding of structure-activity relationship and predictive ADMET.

iNovacia offers a complete coverage of early drug discovery steps from assay development to optimized leads and IND state. Services include assay development, high-througphut screening (HTS), fragment-based screening by NMR and SPR, analytical chemistry, medicinal chemistry at all stages up to lead optimization, ADMET profiling and biophysical characterization of proteins and compound-protein interactions.

iNovacia scientists are using a range of biophysical techniques to decipher and validate mechanism of actions of hit series from HTS The picture shows the high field NMR-laboratory.

The iNovacia HTS compound collection is of highest international standard, validated by several pharmaceutical companies. It consists of ca 280,000 compounds stored in DMSO stock solutions under nitrogen at +4°C. To enhance downstream success all compounds are carefully selected by experienced medicinal chemists applying more than 70 filters to include and exclude desired and undesired properties, respectively. To enable an early SAR already from primary screening the library is designed so that it includes a balanced number of analogues around each scaffold.

The highly experienced HTS team has performed screening campaigns towards all major target classes (GPCRs, ion channels, enzymes, nuclear receptors) using a wide range of assay read-outs (e.g. radioactivity, fluorescence, luminescence, absorbance). Primary fragment screening is performed by ligand-based NMR techniques or SPR using a 900+ fragment library.

The hit-to-lead phase where the most promising hit series are selected for further development in full medicinal chemistry programs is a crucial step for a successful drug discovery project. iNovacia devotes much efforts to ensure that the medicinal chemists work on the most promising hit series. Counter assays and orthogonal assays are employed and our medicinal chemists evaluate the hit series with respect to chemical tractability, library expansion tractability, emerging SAR and IP space. Whenever possible, biophysical assays are performed on hit series representatives in order filter out series active via an undesired mechanism and also to obtain more information on binding modes of compounds from promising hit series. Further, analogues are tested and selected series are expanded by parallel chemistry. Finally, early in-vitro ADME assays are performed before the final prioritization of hit series and continuation of the project into the lead-generation and lead-optimization phases.

iNovacia has several modular service offerings that can be used separately or combined. A combination of the modular offerings can for example cover all steps from assay development to the hit-to-lead phase. iNovacia brings an integrated drug discovery organization underpinned by an investment of 10 Mio EUR in instruments and over 15 years of industrial track record of delivering drugs into the clinic and onto the market.

For further information on iNovacia, please visit the website at:
http://www.inovacia.se
or send an email to
info@inovacia.se

 


Editor

Gabriele Costantino
Univ. of Parma, IT

Editorial Committee

Erden Banoglu
Gazi Univ., TR

Lennart Bunch
Univ. of Copenhagen, DK

Leonardo Scapozza
Univ. of Geneve, CH

Wolfgang Sippl
Univ. Halle-Wittenberg, DE

Sarah Skerratt
Pfizer, Sandwich

Executive Committee

Gerhard F. Ecker President
Roberto Pellicciari Past Pres.
Koen Augustyns Secretary
Rasmus P. Clausen Treasurer
Javier Fernandez Member
Mark Bunnage Member
Peter Matuys Member

For more information please contact info@efmc.info

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