Kinase Screening Library

Nowadays, kinase modulators have gained lots of attraction in drug discovery: more than 50 protein kinase inhibitors are currently approved drugs, and hundreds of them are in clinical trials. Moreover, the number of protein kinase inhibitor chemotypes has increased dramatically over the past decade.

BOC Sciences has built its proprietary kinase screening library using the advanced standards, aiming to screen out a wide range of kinase inhibitors.

Figure 1. Strategy for screening a kinase specific compound library in multidrug resistant osteosarcoma cell lines. (Zhen, D.; et al. 2014)

Kinase Screening Library Design

We employ approximately 1,000 structures and pharmacophore models of known kinase inhibitors obtained from various commercial databases to design our library.

1. Firstly, a 2D fingerprint similarity search is performed against the BOC Sciences HTS compound collection to select nearly 3,000 potential inhibitors and activators for drug-like screening compounds that target key kinases
2. Information on the closest homologs with their highest activity from the database is then collected and added to the information file for each compound
3. Finally, the resulting screened compounds are further filtered through an internal filter to remove PAINS, toxic substances and reactive fractions

Our unique library contains the following kinase inhibitors:

• Inhibitors of protein kinases: ACVRL, ABL, ADK, AKT, ALK, AMPK, Aurora, ATM, AXL, Bcr-ABL, βARK1, Braf, BMX, BRK, BTK, CAMK, CDK, CDC7, CqsS, cFMS, CHK, CK, CNKSR1, cKIT, cMET, CLK, CPK, DAPK, DNA-PK, DYRK, EEFK, EGFR, EPH, erbB, FAK, FLT3, Fyn, GRK, GSK, HK, HPK, HER, JAK, JNK, IGFR, IKK, ILK, IRE, IRAK, ITK, KDR, LCK, luxN, LIMK, LRRK, MAPK, MEK, MELK, MLCK, mTOR, p38α, PAK, PASK, PDPK, PDGF, PIK, PIM, PIP, PGK, PKA, PKC, PFK, PFMRK, PKM2, PLK, PknB, PRKACA, PRMT, RAF, RET, RIPK, ROCK, RTK, SH2, SAPK, SRC, S6K, SKSphK, SPHK, SYK, SGK, TAO, Tie2, TGFB, TK2, TRPM, Trk, TTSP, VEGFR, ZAP-70
• ATP-competitive inhibitors
• DGF-out and αC-helix out non-ATP competitive inhibitors
• MEK non-ATP competitive inhibitors
• Covalent kinase inhibitors
• Allosteric kinase inhibitors
• Kinase activators: AMPK, ABL, DPK1, PKM2

Kinase Screening Library Characteristics

• The comprehensive kinase screening library contains a wide range of selective and non-selective kinase inhibitors, including inhibitors of various lipid, receptor and non-receptor tyrosine, serine/threonine and dual specificity kinases
• Compared to kinase focused library, our kinase screening library provides better coverage of individual kinases, kinase isoforms and mutants, and kinase families
• 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 Kinase Screening Library design at competitive prices for global customers. Personalized and customized services of 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!