I’m attending the 17
th RSC/SCI Medicinal Chemistry conference in Cambridge at the moment.
We’ve had some fantastic talks, including a really provocative and thought-provoking talk from
Chas Bountra at the
Structural Genomics Consortium on a new model of pre-competitive collaborations between industry and academia as a way to reduce Phase II attrition.
But that’s not what I want to talk about. We’ve had a lot of really interesting talks on improving the properties of drugs to improve success. For example,
Tim Ritchie talked about all the parameters we used to asses compounds (LogP, LE, LLE, MW, PSA etc. etc.) and debated which of these should we actually use to guide our decisions and when. He
concluded that PFI and Fsp3 are some of the most generally applicable ones, which is in agreement with a recent
paper from Michael Shultz (which is well worth a read).
We also had a talk from
Simon Hodgson about the importance of solubility (and why, even though we all know it’s important we still make insoluble compounds!). However, these talks were followed by this beast from
Gilead:
This compound is in various
Phase III trials. It works, somehow!
This is why I love medicinal chemistry. If any of us knew what we were doing, if any of the “rules” worked, the robots would have taken over long ago!