Properties and Drug Quality

Library design for HTS INTESTINAL PERMEABILITY VI. METABOLIC STABILITY 

Poor solubility and library C. Intramolecular hydrogen culture 

Importance of the D. Permeability testing permeability assay noise 

If protocol development is rate A. The definition of poor VII. ACCEPTABLE SOLUBILITY 

Poor ADME properties - B. Aqueous solubility and blunt PERMEABILITY SCREENS 

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Lipinski CA and Hoffer E. Compound Properties and Drug Quality. Practice of Medicinal Chemistry (2nd Edition) 200, pp. 341—349. 

Product quality often cannot be defined quantitatively. In some processes, however, product quality and its reproducibility are paramount. Examples would include surface finishing, where it is of overriding importance that the surface has the desired appearance or properties, and drug manufacture, where the absence of even trace amounts of some impurities can be critical. 

Poor pharmacokinetics and toxicity are important causes of costly late-stage failures in drug development. It is generally recognized that, in addition to optimized potency and specificity, chemical libraries should also possess favorable ADME/Tox and druglike properties [77-80]. Assessment of druglike character is an attempt to decipher molecular features that are likely to lead to a successful in vivo and, ultimately, clinical candidate [81-83]. Many of these properties can be predicted before molecules are synthesized, purchased, or even tested in order to improve overall lead and library quality. 

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