tag:blogger.com,1999:blog-1136153439451224584.post4167517788783005613..comments2024-03-27T06:45:59.174-07:00Comments on Practical Fragments: LigandabilityDr. Teddy Zhttp://www.blogger.com/profile/07288045760981372367noreply@blogger.comBlogger2125tag:blogger.com,1999:blog-1136153439451224584.post-87250140370213081512011-05-10T07:27:36.499-07:002011-05-10T07:27:36.499-07:00Hi Darren,
I agree; nothing beats empiricism!
&q...Hi Darren,<br /><br />I agree; nothing beats empiricism!<br /><br />"Fast follower" is sometimes also called "patent busting." The idea is to take published patent applications from competitors, make some of the best compounds, and then med-chem into novel chemical space. This can be very effective: the current HIV protease inhibitors, for example, are far more effective than the first generation compounds.Dan Erlansonhttps://www.blogger.com/profile/07927082337051189270noreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-7756643493560496032011-05-09T10:24:21.368-07:002011-05-09T10:24:21.368-07:00Hi Dan - This is a nice survey of AZ's interna...Hi Dan - This is a nice survey of AZ's internal FBLD, and like Phil Hajduk's referenced paper, underlines the importance (and advantages) of conducting real experiments as part of target assessment. We tried to use computational tools to predict the likelihood of what we would call "crystallographic ligandability" (see Doug's MIE book chapter). But this method was far from perfect, and never as informative as simply trying new targets out with a subset of our library.<br /><br />Question: what is the "fast-follower" strategy?<br /><br />- dbDarren Begleyhttps://www.blogger.com/profile/08353170982254950962noreply@blogger.com