The Rule of 5 made its entrance about 10 years ago and provided a desperately needed wake up call to a pharmaceutical industry that had been seduced by combinatorial chemistry, high throughput screening and Andersen Consulting (couldn't find hyperlink for them). It is also one of the more sacred cattle in the pasture and will be the subject of our next post. Before we do this, it is appropriate to link material from a couple of others more experienced in the blog trade. Milkshake sensibly notes that Ro5 is fairly crude but points in the right direction. TotallyMedicinal has compiled a list of articles from the literature with the Ro5 paper as the first item, totally in keeping with it's sacred cow status. If you've already blogged about Ro5, make a comment, include the link and be part of the fun!
On the lighter side, we hope that Britain's Queen Elizabeth II is enjoying her visit to the US and note that Dubya and the Duke of Edinburgh really do deserve each other. Apparently The Queen once met a photographer on a state visit to Canada and the ensuing conversation went something as follows:
Q: "A photographer! How very interesting, my brother in law [The photographer Lord Snowdon was married to Her Majesty's late sister at the time] is a photographer".
P: "Ah, how very coincidental! My brother in law is a queen".
On the lighter side, we hope that Britain's Queen Elizabeth II is enjoying her visit to the US and note that Dubya and the Duke of Edinburgh really do deserve each other. Apparently The Queen once met a photographer on a state visit to Canada and the ensuing conversation went something as follows:
Q: "A photographer! How very interesting, my brother in law [The photographer Lord Snowdon was married to Her Majesty's late sister at the time] is a photographer".
P: "Ah, how very coincidental! My brother in law is a queen".
next
2 comments:
My take on the RO5. Lipinski says that less than 10% of drugs fail two of the four calculable tests. What does this mean? I take it to mean that in practical terms a compound can quite happily break one of Lipinski's rules and still have a decent chance of being orally available. ie most people would scream "But what about the RO5!"
And you mustn't forget that the rules dont apply for actively transported drugs **the fifth rule**
Great blog. I do materials chemistry, but I try to keep up (very casually) with what med chemists are up to, because you guys are generally super synthetic chemists, and I'll gleefully steal whatever reactions you discover and try and make molecules for transistors or something out of it.
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