Creative Biostructure

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MagHelix™ Hit to Lead

With a dedicated team of skilled scientists and technicians, Creative Biostructure provides MagHelix™ hit evaluation and lead identification (hit to lead) services to meet our clients’ needs and goals. Our MagHelix™ service platform includes secondary assays, specificity assays, dose response curves, Intellectual property (IP) assessment as well as studies of chemical amenability and mode of action.

Secondary assays: They are able to validate hits, identify the lead and evaluate the improvement of structural and pharmacokinetic properties following lead optimization. Our seasoned scientists can develop a panel of secondary assays via biochemical, biophysical and cell-based assays. Of these, biochemical assays provide orthogonal confirmation and validation; biophysical assays detect the binding affinities between a hit and the target by Nuclear Magnetic Resonance (NMR), Isothermal Titration Calorimetry (ITC), Dynamic Light Scattering (DLS), and Surface Plasmon Resonance (SPR) techniques; cell-based assays, on the other hand, are used to analyze the effectiveness and specificity of a hit in cells of customers’ interest.

Specificity assay: It is essential to validate a candidate hit by the specificity assays, which also filter out the non-specific and promiscuous inhibitors.

Dose response curves: They describe the relationship between the dose and effect of a compound. These curves can be used to quantitively measure the activities of a hit against the target and their binding interaction (e.g., IC50 or EC50).

Intellectual property (IP) assessment: It checks the novelty against documented patents of hit structures in specialized databases.

Chemical amenability: Our scientists can assess the amenability of a hit based on its structure as well as feasibility of synthesis and process development, including up-scaling and costs.

Mode of action: Creative Biostructure can explore and determine the mechanism of action for enzymes, inhibitors, and receptor agonists/antagonists. We also can characterize binding kinetics and binding sites by assays such as X-ray crystallography, Electron Microscopy (EM) and NMR.

With biochemical, biophysical and cell-based assays, Creative Biostructure can facilitate hit-to-lead processes and meet the needs of customers with our tailor-made services.

Creative Biostructure supplies the following MagHelix™ In vitro assay services that will benefit your projects:

Assay Development

  • Assay technologies

Library Design and Screening

  • Targets
  • Targeted diseases
  • Library screening

Hit to Lead

  • Hit evaluation and lead identification
  • Mode of action
  • X-ray Crystallography
  • Customized NMR services

ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) Modeling and Profilling

Natural Products