A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.

@article{Auld2009ABF,
  title={A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.},
  author={Douglas S Auld and Ya-qin Zhang and Noel T Southall and Ganesha Rai and Marc J. Landsman and Jennifer MacLure and Daniel Langevin and Craig J. Thomas and Christopher P. Austin and James Inglese},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 5},
  pages={1450-8}
}
We measured the "druggability" of the ATP-dependent luciferase derived from the firefly Photuris pennsylvanica that was optimized using directed evolution (Ultra-Glo, Promega). Quantitative high-throughput screening (qHTS) was used to determine IC(50)s of 198899 samples against a formulation of Ultra-Glo luciferase (Kinase-Glo). We found that only 0.1% of the Kinase-Glo inhibitors showed an IC(50) < 10 microM compared to 0.9% found from a previous qHTS against the firefly luciferase from… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 24 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 44 references

Bioluminescent assays for ADMET.

Expert opinion on drug metabolism & toxicology • 2008

Similar Papers

Loading similar papers…