Inhibition profiling of human carbonic anhydrase II by high-throughput screening of structurally diverse, biologically active compounds.

@article{Iyer2006InhibitionPO,
  title={Inhibition profiling of human carbonic anhydrase II by high-throughput screening of structurally diverse, biologically active compounds.},
  author={Rema Iyer and Albert A Barrese and Shilpa Parakh and Christian N. Parker and Brian C Tripp},
  journal={Journal of biomolecular screening},
  year={2006},
  volume={11 7},
  pages={782-91}
}
Human carbonic anhydrase II (CA II), a zinc metalloenzyme, was screened against 960 structurally diverse, biologically active small molecules. The assay monitored CA II esterase activity against the substrate 4-nitrophenyl acetate in a format allowing high-throughput screening. The assay proved to be robust and reproducible with a hit rate of approximately 2%. Potential hits were further characterized by determining their IC(50) and K(d) values and tested for nonspecific, promiscuous inhibition… CONTINUE READING
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