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.
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|
|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|
|Natural Products Library NPL-720||TimTec||720|
|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.