Small-molecule kinase inhibitors: an analysis of FDA-approved drugs.

@article{Wu2016SmallmoleculeKI,
  title={Small-molecule kinase inhibitors: an analysis of FDA-approved drugs.},
  author={Peng Wu and Thomas E. Nielsen and Mads H Clausen},
  journal={Drug discovery today},
  year={2016},
  volume={21 1},
  pages={5-10}
}
Small-molecule kinase inhibitors (SMKIs), 28 of which are approved by the US Food and Drug Administration (FDA), have been actively pursued as promising targeted therapeutics. Here, we assess the key structural and physicochemical properties, target selectivity and mechanism of function, and therapeutic indications of these approved inhibitors. Our analysis showed that >30% of approved SMKIs have a molecule weight (MW) exceeding 500 and all have a total ring count of between three and five. The… CONTINUE READING
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