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Medicinal Chemistry – Hit2Lead

Facility part of the DDD platform

 

Medicinal Chemistry Hit2Lead is a facility belonging to the Drug Discovery and Development platform (DDD) at Science for Life Laboratory (SciLifeLab). We design and synthesize new compounds to accelerate academic drug discovery projects with the aim to identify a compound with a promising profile for proof-of-concept animal studies. Drug discovery is a complex area and to be successful we need to understand the underlying cause of the disease and evaluate the potential and limitations with the different compounds we prepare. We do this in collaboration with the other facilities at SciLifeLab DDD. We work closely together with our chemistry colleagues in Uppsala.

 

 

“We can analyze and evaluate compounds.We can design and prepare new compounds. We have experience of drug discovery compounds.

We are medicinal/computational/organic chemists and are here to catalyze you research in drug discovery.”

*Or “molecules”, “drugs”, “active substances”, “chemicals”, “screening hits” etc. It does not matter. We work with them all.

 

 

 

As part of a new modality initiative within DDD a PROTAC technology platform has been initiated at the Hit2Lead facility. Modulating diseases by small molecules has historically been limited to either inhibition or activation of biological targets. With the new PROTAC technology it is possible to degrade a target (stop its activity completely) by hijacking the endogenous ubiquitination pathway.

A toolbox with different E3-ligase and linkers will be finished during 2020 that will enable fast evaluation if a PROTAC approach is applicable to modulate the target of interest.

 

 

We want to collaborate with you. The initial hit compound showing activity at your target can be obtained through e.g. fragment-based drug discovery (FBDD) technologies, rational drug design, or from high-throughput screening (HTS) capabilities available at SciLifeLab via CBCS etc. Please contact us for a discussion around your ongoing research.

SERVICES

  • Access to >200.000 compounds for screening
  • Organic synthesis of bioactive small molecules
  • High-speed synthesis capabilities
  • Compound characterization, structure determination and purity analysis
  • Separation of enantiomers on a preparative scale
  • Medicinal chemistry expertise
  • Design and synthesis of analogues to expand hit series
  • Selection and purchase of compounds to make a hit more lead like (more likely to have the potential to successfully be developed into a drug)
  • Prioritization of compounds for proof-of-concept animal studies
  • Competitive intelligence discussions (Intellectual Property [IP], patents, immaterial rights etc)
  • Molecular Modelling and Computer-based drug design
  • Quantitative structure-activity relationships (QSAR) and cheminformatics
  • Virtual screening

EQUIPMENT

  • A laboratory equipped for organic synthesis
  • Access to a large amount of chemical reagents
  • Microwave reactor
  • H-Cube mini for flow hydrogenation
  • Automated flash chromatography systems
  • Preparative HPLC instruments (including an SFC for chiral separation)
  • NMR spectrometer
  • Analytical LC-MS
  • Small-molecule drug discovery and protein modeling software suits
  • High-level computational in-house capacity