tag:blogger.com,1999:blog-1136153439451224584.post525981609114122953..comments2024-03-27T06:45:59.174-07:00Comments on Practical Fragments: Like the Elves to Valinor?Dr. Teddy Zhttp://www.blogger.com/profile/07288045760981372367noreply@blogger.comBlogger7125tag:blogger.com,1999:blog-1136153439451224584.post-89570416243679243602014-08-28T16:59:59.253-07:002014-08-28T16:59:59.253-07:00Teddy -- I said "avidly". I have seen t...Teddy -- I said "avidly". I have seen teams (internal and at potential "partners") optimize "potency" without regard to functional effects. <br /><br />Delivering a potent ligand of absolutely no use to me.<br /><br />I really don't care who makes the molecules, or who drives the project. Someone needs to keep their eye on the ball.<br /><br />(I vehemently disagree with the comment above that "no single person has the expertise . . . to unilaterally make decisions on the direction the project takes" BTW. I know several such people. Rare, true, but not unknown.)<br /><br />Anonymousnoreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-8350452314713865372014-08-28T13:34:55.101-07:002014-08-28T13:34:55.101-07:00@Anonymous, why would you expect a weakly binding ...@Anonymous, why would you expect a weakly binding compound to necessarily have a functional effect? Dr. Teddy Zhttps://www.blogger.com/profile/07288045760981372367noreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-78444645996622213482014-08-28T13:28:21.352-07:002014-08-28T13:28:21.352-07:00More and more, particularly in PPI targets, I am s...More and more, particularly in PPI targets, I am seeing project teams come forward with molecules that bind avidly to the target protein. The biophysicists and CADD guys (and gals) are justifiably proud of their contributions,<br /><br />Unfortunately, too often, these molecules do nothing functionally, and thus are essentially useless as starting points for a drug discovery project. A (decent, or at least trained by me) medicinal chemist would have asked that question up front.<br /><br />So, there is still education to be imparted, on both ends. As noted above, "most important" misses the point. Anonymousnoreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-4095294882015508992014-08-21T06:47:49.012-07:002014-08-21T06:47:49.012-07:00I always think discussion about who is the most im...I always think discussion about who is the most important is missing the point. You can be as great a Med Chemist or Biophysicist as you like, but no one single person has the expertise in biology, chemisty, biophysics, assay dev, DMPK, safety etc to be able to unilaterally make decisions on the direction the project takes. I really think our industry has struggled over the past two decades because Medicinal Chemists ruled the roost to the detriment of other equally skilled scientists in other fields. I think it would be equally foolish for biophysicists to assume they can replace medicinal chemists in this role. <br /><br />For me the key to successful drug discovery is team work, humility and knowing where the limits of your knowledge are.Anonymousnoreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-66266674813794698452014-08-21T05:14:28.719-07:002014-08-21T05:14:28.719-07:00Derek comments on it: http://pipeline.corante.com/...Derek comments on it: http://pipeline.corante.com/archives/2014/08/21/fragonomics_eh.phpDr. Teddy Zhttps://www.blogger.com/profile/07288045760981372367noreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-61194347047450235322014-08-21T03:56:04.363-07:002014-08-21T03:56:04.363-07:00Not saying they aren't essential. I am saying...Not saying they aren't essential. I am saying the need for their engagement has been pushed back in the whole process, thereby easing a resource crunch early in the process and putting them later where they have more impact.Dr. Teddy Zhttps://www.blogger.com/profile/07288045760981372367noreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-42126254651476182992014-08-20T20:26:48.600-07:002014-08-20T20:26:48.600-07:00Much as I'd like to visit Valinor, I'd say...Much as I'd like to visit Valinor, I'd say that medicinal chemists are still just as essential today as they ever have been. Not only are we needed to design libraries and avoid PAINS, it's pretty difficult to transform a millimolar fragment to a lead - let alone a drug - without medicinal chemistry!Dan Erlansonhttps://www.blogger.com/profile/07927082337051189270noreply@blogger.com