Chemistry-driven target discovery

Chemistry-Driven Target Discovery Enabling Biology 165 4.2... 

Chemistry-Driven Target Discovery Enabiing Bioiogy 169... 

Figure 4.1 Chemistry-driven target identification by phenotypic screening fit in the drug discovery value chain (boxed). Some discovery activities could (should, whenever possible) be prosecuted in parallel.

Without a doubt each company s compound collection will be biased in favor of structural classes they ve invested in most heavily over the years. But the preponderance of target-directed drug discovery projects being a relatively recent phenomenon, many of the medchem compounds in such collections arose from more chemistry-driven considerations. Consequently, they tend to be relevant to a range of different biological targets, which may or may not have been appreciated when they were made. 

Advances in identification of therapeutic targets and medicinal chemistry to interact with these targets have driven changes in the way that toxicologists contribute to the discovery and development of drugs. The emphasis is... 

The SAR of the bisacylhydrazines, both during and after the discovery of the commercial compounds, has been extensively studied. This was partly driven by the novelty of the chemistry, mode of action (ecdysone agonists via interaction with the ecdysone receptor), and the availability of suitable assays (tissue, cell and target site based). Numerous papers have been published on this subject and the reader is referred to an excellent review by Dinan and Hormann [6] as a starting point. This section highlights and summarizes the collective findings by various researchers. 

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