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Drugability

In modern drug discovery speed and cost control are important in addition to high quality. In silica virtual screening for drugability [159] is a good first step in library... [Pg.42]

In this book, a conceptually rigorous effort was made to describe the state-of-the-art physical methods that underlie the processes related to absorption. The aim was to give conceptual tools to the analytical chemists in pharmaceutical companies who do such measurements, so that they could in turn convey to the medicinal chemists, who make the molecules, how structural modifications can affect those physical properties that make candidate molecules drugable. ... [Pg.249]

Figure 2.2 BioPrint assays (cyan) mapped onto the drugable proteome. Figure 2.2 BioPrint assays (cyan) mapped onto the drugable proteome.
Much of the skepticism as to the drugability of kinases was assuaged by the development of imatinib (Gleevec Novartis, Basel,... [Pg.208]

Lead compounds that survive the initial screening are then optimized or altered to improve their drugability and developability (that is, they are developed to achieve better physicochemical and biopharmaceutical properties and more effective and safer profiles in animals). Scientists make and laboratory-test hundreds of different variations or analogs of the initial lead compounds to evaluate the structure-activity relationship (SAR) of the hits. [Pg.7]

The word drugability is often used to cover all aspects of a molecule beyond initial potency. A potential drug compound must overcome many challenges in order to be a successful therapeutic. Critical components of drug design include absorption, permeation, distribution, metabolism, stability, specificity (does it do more than... [Pg.105]

A common approach to lead optimization is now parallel optimization, which is discussed in the following section. This is an extremely challenging undertaking because it requires the simultaneous control of several medicinal chemistry components. Furthermore, many of these components are not independent and, in fact, may even be negatively correlated. To do parallel optimization, it is also necessary to generate drugability related information in the early stages of lead optimization. [Pg.109]


See other pages where Drugability is mentioned: [Pg.54]    [Pg.72]    [Pg.223]    [Pg.7]    [Pg.23]    [Pg.29]    [Pg.29]    [Pg.410]    [Pg.443]    [Pg.15]    [Pg.18]    [Pg.62]    [Pg.97]    [Pg.176]    [Pg.180]    [Pg.69]    [Pg.11]    [Pg.10]    [Pg.131]    [Pg.585]    [Pg.552]    [Pg.5]    [Pg.27]    [Pg.175]    [Pg.105]    [Pg.437]    [Pg.437]    [Pg.62]    [Pg.91]    [Pg.91]    [Pg.92]    [Pg.93]    [Pg.94]    [Pg.94]    [Pg.95]    [Pg.96]    [Pg.98]    [Pg.102]    [Pg.176]    [Pg.177]    [Pg.210]    [Pg.231]   
See also in sourсe #XX -- [ Pg.5 ]

See also in sourсe #XX -- [ Pg.105 ]

See also in sourсe #XX -- [ Pg.357 ]

See also in sourсe #XX -- [ Pg.47 ]

See also in sourсe #XX -- [ Pg.66 ]




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