HIT Screening by

Thrombotargets has developed a novel and innovative approach to traditional HTS that will change the way lead compounds are identified in the areas of Hemostasis, Atherosclerosis, Aging and Thrombosis

HIT Screening by
Lead Optimization and Evaluation
Preclinical and Clinical Development

HIT Screening by

 

The main relevant characteristics of   are:

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1. No interferences with biological matrix.

Using human matrix, avoids testing a target on a strange matrix (buffers, culture medium, etc).

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2. Capable to evaluate pathways instead of single targets, rendering therefore simultaneously multiple HITS for different targets. 

In classical HTS we are able to evaluate the binding of small molecules on a defined Target rendering only one Lead, this approach could be defined as

 

“ONE TARGET ASSAY” 

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“ONE LEAD”

 

  is able to evaluate the effect of small molecules on a defined Pathway, rendering several Leads for several Targets. We define our approach as:

 

 

 

 

 

"ONE PATHWAY ASSAY"

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"SEVERAL TARGETS"

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"SEVERAL LEADS"

 

3. High value biological information

  • Provides biological activity instead of binding information.
  • Detects all the targets involved in the response
  • Identifies new targets related to the analyzed activity

4. Provide efficient screening tools to therapeutic areas classically deprived of HTS.

 

   Screening Focus :

  • Coagulation (pro and anti)
  • Fibrinolysis (pro and anti)
  • Antioxidants
  • Antiatherosclerotic (LDL peroxidation inhibitors)

 

5. Ex vivo information useful to drive successfully clinical trials (Phase I, Phase II and Phase III)

For the first time, a Drug Discovery Screening Platform as provides ex-vivo information useful to drive successfully all the Clinical Phases:

  • On human healthy-like conditions and estimated dose useful to drive successfully Clinical Phase I
  • On patient-like conditions and efficiency of the compound useful to drive successfully Clinical Phase II
  • Comparative efficiency information of the compound vs gold-standard treatment useful to drive successfully Clinical Phase III

 

6. Screening Capacity at the level of ultra HTS that enables the screening of over 40 million compounds per year. 

Efficient platforms that are able to work at ultra HTS level. The screening capacity is of over 40 million compounds per year and the platforms can use 96-, 384-, and 1536-well formats. 

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7. Types of  platforms:

  • Hemosta

Thrombotargets has developed and adapted to High Throughput Screening a whole Hemostasis Pathway Assay named HemostaScreen, capable to simultaneously quantify clot formation and clot lysis. In this way, with this   we can simultaneously evaluate the effect of small molecules on Coagulation and on Fibrinolysis.

  • Oxidant

can evaluate the antioxidant effects of small molecules by means of determining their effect on the total antioxidant capacity. This platform is also specific to the oxidant process associated with neurodegenerative diseases and aging

  • Athero

  can evaluate the antiatherosclerotic effect of small molecules by means of inhibiting the modification of low-density lipoproteins (LDL) by lipoperoxidation. 

 

 

 

 

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