Tyrosine Kinase Screening Library

Tyrosine kinases (TKs) belong to a relatively complex class of enzymes that emerged at an early stage of evolution, and are involved in phosphorylation and dephosphorylation of proteins together with protein phosphatases. TKs are key molecules in signaling pathways and important targets in drug discovery. There are two types of tyrosine kinases in cells: receptor tyrosine kinases and non-receptor tyrosine kinases. The main roles of TKs include regulation of multicellular functions of the body. Intercellular signals related to growth, differentiation, adhesion, motility, and death are usually transmitted via tyrosine kinases. Tyrosine kinases are attractive biological targets for cancer therapy because their abnormal signaling is often associated with tumor development and growth.

BOC Sciences can design a new tyrosine kinase screening library containing approximately 5,700 drug-like screening compounds for high-throughput screening (HTS).

Tyrosine Kinase Screening Library Design

1. Firstly, approximately 150,000 reference compounds with known TKs blocking activity are obtained from a variety of commercial databases
2. Then, these compounds are initially filtered to retain only those with moderate and high activity against TKs
3. In the next step, we perform a 2D fingerprint similarity search against the reference set to analyze the BOC Sciences HTS compound collection
4. Finally, the compounds obtained will be further filtered using Lipinski's Rule of Five to deliver only drug-like ones. In addition, PAINS compounds and compounds with reactive groups are removed from the library

At BOC Sciences, the generated potential tyrosine kinase inhibitors possess activity against the following targets:

Figure 1. A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors. (Lotz-Jenne, C.; et al. 2016)

Tyrosine Kinase Screening Library Characteristics

• High diversity over the screening set: mean Tanimoto > 0.85
• Favorable physicochemical parameters and solubility requirements
• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Bioactivity and safety confirmed by preclinical studies and clinical trials
• Structural diversity, medicinal activity, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• All compounds are continually updated
• Compound cherry-picking service is provided

What We Deliver

• Delivered within 2 weeks in any customer-preferred format
• Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
• All compounds have a minimum purity of 90% assessed by ¹H NMR and HPLC
• Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Tyrosine Kinase Screening Library design at competitive prices for global customers. Personalized and customized services of Tyrosine Kinase Screening Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!