Lipinksi Rules, Biotech Bootcamp and Sharktank

“Yes, I’m sure that’s what Watson and Crick thought when they worked on the structure of DNA. Who’s going to buy this thing?”

The Confluence

Back about 20 years ago, a medicinal chemist named Lipinski came up his “Rule of Five” for whether a chemical compound had “drug like properties”. Never mind what they are, unless you’re planning to start a lab in your garage. There have been variations on the “rule of five”, like, do you really need a drug right out of the starting gate? Why not look for lead-like compounds? What are the properties of those? And how did you come up with these rules anyway?

The bottom line answer is, well, after you’ve seen a bajillion compounds coming out of high throughput screening and have worked on thousands more, you just know. You can look at a compound and say, ehhhh, that’s never going to be a drug. The tailpiece has too many carbons or the scaffold is too skimpy or that compound is promiscuous. (Um, that’s as sexy as drug…

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