The impact of aromatic ring count on compound developability: further insights by examining carbo- and hetero-aromatic and -aliphatic ring types.

@article{Ritchie2011TheIO,
  title={The impact of aromatic ring count on compound developability: further insights by examining carbo- and hetero-aromatic and -aliphatic ring types.},
  author={Timothy J. Ritchie and Simon J. F. Macdonald and Robert J Young and S. D. Pickett},
  journal={Drug discovery today},
  year={2011},
  volume={16 3-4},
  pages={164-71}
}
The impact of carboaromatic, heteroaromatic, carboaliphatic and heteroaliphatic ring counts and fused aromatic ring count on several developability measures (solubility, lipophilicity, protein binding, P450 inhibition and hERG binding) is the topic for this review article. Recent results indicate that increasing ring counts have detrimental effects on developability in the order carboaromatics≫heteroaromatics>carboaliphatics>heteroaliphatics, with heteroaliphatics exerting a beneficial effect… CONTINUE READING

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