Primary Screening

Primary Screening

High-throughput screening of a compound library is often the first step in a drug discovery project seeking to create a small molecule for inhibition of the activity of a target protein. Reaction Biology has developed the HotSpot screening format for high-throughput screening of kinase and methyltransferase inhibitors. This miniaturized radiometric assay enables robust low-volume testing of enzymatic activity. 

Fragment libraries can be screened at Reaction Biology with the capacity of our high-throughput capable 8K+ Biacore machines via surface plasmon resonance spectrometry (SPR). 

Advantages of The Reaction Oncology Platform:

  • Get a head start for your drug discovery project by a large palette of established assays that are ready to use for high-throughput screening.
  • A variety of counter and orthogonal screening options allows fast verification of hits.
  • Our medicinal chemistry partners will help to elucidate if the structure of the hits shows any promise for further progress.

Our primary screening options include radiometric, fluorescent, or colorimetric assays as well as thermal shift binding assays and surface plasmon resonance. Reach out to us today and we will be happy to discuss options for your primary compound screen.

Libraries

Reaction Biology offers the following compound libraries for high-throughput screening. Clients are welcome to provide other compound libraries for primary screening.

Name Vendor Number of Compounds
DIVERSet-CL Library Chembridge 50.000
Maybridge HitCreator FisherSci/Maybridge 14.200
Diversity Screening Set Life Chemicals 50.240
FDA-approved Drug Library SelleckChem 2.701
Kinase Inhibitor Library SelleckChem 1.802
2018 FDA-approved Mini Library  SelleckChem & MedChem Express 50
PPI Fragments Life Chemicals 3.873
Ultimate Fragment Library Selection Life Chemicals 1.000

The Creation of Hit Series

Symeres routinely applies an array of computational tools to evaluate hit series obtained from a high throughput screening or virtual screening campaign. Hit series are clustered and triaged and assigned a ‘lead-like’ score based on activity, physicochemical properties, synthetic accessibility, and chemical novelty (IP).

In addition, in structurally enabled programs, modeling and docking tools are employed to validate hits and evaluate possible binding modes.