KINOMEscan: Kinase Binding Assay Platform

Why KINOMEscan®?

Industry trusted technology that has supported multiple IND filings for clinical candidates and drug approvals and continues to advance kinase drug discovery.

What is KINOMEscan?

High throughput site-directed competition affinity binding assay for rapid characterization of your molecules in over 500 kinase domain-containing human wild-type and clinically relevant mutant targets.

Video explaining technology principle behind KINOMEscan.
 

Benefits of KINOMEscan:

  • Adaptability to screen multiple modalities (small molecules, peptides, conjugate therapies) to evaluate Type I and Type II kinase catalytic domain inhibitors, covalent inhibitors, and bifunctional degraders
  • Rapid Turn-Around Time and Auto-Escalation for supporting AI and machine learning research projects
  • TREEspot® Data Visualization tool with customizable reports
  • Custom Assay Development for your domain of interest

 

TREESpot Visualization

TreeSpot Visualization
BTK Inhibitor Selectivity TREEspot Visualization depicts kinase panel hit profile for remibrutinib (on the left), the most selective BTK inhibitor, and nemtabrutinib (on the right), the least selective BTK inhibitor, as red dots on a phylogeny of kinases. Dot size indicates hit strength, so the larger the red dot, the stronger the hit.

Key Drug Targets within KINOMEscan:

  • JAK/STAT
  • BTK/PLCγ/PKC
  • RAS/RAF/MAPK/MEK (ERK, JNK, p38)
  • PI3K/AKT/mTOR
  • Wnt/β-catenin

 
 

Key Areas

The largest commercial kinase panel available, scanMAX contains a set of 468 kinases covering AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid and atypical kinase families, plus important mutant forms.

An economical approach to surveying the human kinome, scanEDGE includes 97 kinases distributed throughout the AGC, CAMK, CMGC, CK1, STE, TK, TKL, lipid, and atypical kinase families, plus important mutant forms.

scanTK is the largest commercial panel of tyrosine kinases that includes a set of 135 both receptor and non-receptor kinases, plus important mutant forms.

scanELECT is an extremely flexible solution with multiple applications including, primary HTS & lead discovery and ongoing lead optimization & SAR.

Quantitate compound binding affinity against any kinase assay. Inhibitor binding constants (Kd values) are calculated from duplicate 11-point dose-response curves.

Quantitate compound binding affinity against the entire panel of KINOMEscan kinase assays. Inhibitor binding constants (Kd values) are calculated from duplicate 11-point dose-response curves (plus DMSO control).

Kinase activation is often driven by the phosphorylation of residues in key regulatory elements, including, among others, the activation loop (A-loop) and receptor tyrosine kinase (RTK) autoinhibitory juxtamembrane (JM) domains.

Features