Escape from flatland: increasing saturation as an approach to improving clinical success.

By F. Lovering, J. Bikker, Christine Humblet. 2009

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Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles (2010, result): “This metric is similar to the recently reported Fsp(3) metric (14); again, this metric is size-independent, varying on the range [0,1] for each molecule.”
SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules (2017, neutral): “The latter is inspired from commonly accepted bioavailability and drug-likeness guidelines 23,24 .”
Lipophilicity in drug discovery (2010, background): “Along these lines, it has been suggested that reduction of molecular weight [21,35,40], removal of aromatic rings [75] and increased saturation or added chirality [76] might offer generic means of achieving this.”
Resistance of Gram-Negative Bacteria to Current Antibacterial Agents and Approaches to Resolve It (2020, background): “Metal compounds have unique modes of action, and exist in a wider range of three-dimensional geometries, a feature that is associated with higher clinical success rates compared to the generally flat organic molecules [85,86].”
Molecular obesity, potency and other addictions in drug discovery (2011, background): “drug discovery process is enhanced by an increase in the fraction of sp3 hybridized carbon atoms and the number of chiral centers present [9].”