Hit to Lead

Our Hit to Lead Workflow

Comprehensive Plant Natural Compound Library

1.

HIT Generation


Modern drug discovery campaigns need to include natural products to enhance the realm of chemical structures and to obtain qualified drug-like compounds. Intelligent screening with Bicoll Plant Profiles™ provides a rich reservoir of structural diversity and high biological activity potential balanced by costs, time, and quality. The ideal starting point for the hit to lead workflow.

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1. INTELLIGENT SCREENING

Bicoll generates high potential Plant Profiles™ from crude extracts using a proprietary separation system BIFRAC N. The results are fine fractions that pre-qualify compounds based on properties. This allows for a cost- and time-effective screening process even for restricted budgets. Bicoll libraries include a wide range of novel chemical structures, which were hardly possible to identify from extracts before. Bicoll offers approximately 600 unique compounds from each plant organ.

Bicoll plant Profiles™ are ready to use in screening assays, including HTS. In only two rounds of screening, active agents can be identified and thereafter, structure elucidated. This represents significant cost savings as compared to expensive pure natural product libraries. Most elucidated structures are within a molecular weight range of 350 to 450 Da.

2. Natural Product Chemistry

Innovative techniques, methods and equipment bring qualified leads into drug discovery projects. Our experienced international team provides ideas and services tailored to client specific needs:

  • development of novel deconvolution and isolation strategies to speed up access to unique sets of compounds.
  • guarantee rapid structure elucidation to keep projects in time.
  • know-how for fast and easy scale up for re-delivery of larger compound amounts.
  • guidance through all steps of the drug discovery process: From hit generation over Lead Generation to Lead Optimization.

2.

LEAD GENERATIOn

medicinal chemistry hit to lead molecule


Bicoll’s proprietary high throughput prediction toolbox  BIPRESELECT™ reduces the attrition rate of potential drug candidates, which progress through development and the hit to lead workflow. Identification and exclusion of problematic compounds up-front and in this step is crucial to significantly lower screening cost and increase productivity.

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This Natural Product (NP) hit confirmation and validation foresee fast conversion into qualified lead series. Therefore the assessment of physicochemical and pharmacological properties has to be conducted at very early stages of drug discovery. Accelerated conversion of hits into leads and then into qualified development candidates support successful lead generation. Lead Optimization proceeds with the development of mentioned properties.

3.

Lead OPTIMIZATION

Optimizing Lead Compound Hit-to-Lead


Once the structure has been identified, the goal is to enhance the desired properties and to address deficiencies (if any). Lead optimization as the last step in the hit to lead process is focused on analyzing the selectivity and specificity of a compound towards a given target and potential safety concerns. As a result, the promising compound will be confirmed as pre-clinical candidate.

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The goal in lead optimization is to incorporate the best drug characteristics as early on in the process as possible utilizing Bicoll’s unique strategy. This includes the selectivity and specificity towards a given target and potential safety concerns. As a result, the promising compounds will be confirmed as preclinical candidates. The reason is here to improve both the affinity for the target and specific ADME / Tox properties.  

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