tag:blogger.com,1999:blog-1136153439451224584.post4134248112175471898..comments2024-03-27T06:45:59.174-07:00Comments on Practical Fragments: Fragments in Living CellsDr. Teddy Zhttp://www.blogger.com/profile/07288045760981372367noreply@blogger.comBlogger2125tag:blogger.com,1999:blog-1136153439451224584.post-42651603756650114582013-05-08T23:14:13.718-07:002013-05-08T23:14:13.718-07:00Hey thank you guys for your informative (and frequ...Hey thank you guys for your informative (and frequent) posting. I don't work on fragments but I enjoy reading. Hope you keep it going. Anonymousnoreply@blogger.comtag:blogger.com,1999:blog-1136153439451224584.post-1336062538543074522013-05-08T20:53:08.972-07:002013-05-08T20:53:08.972-07:00This is nice, though as with the Heptares paper th...This is nice, though as with the Heptares paper the focus is on potent fragments, with low micromolar (or even high nanomolar!) affinities. That's great if such fragments exist, which (as Teddy points out) is likely to be the case for many GPCRs. However, for more difficult targets such as the Class B GPCRs it is hard to find any tight-binding small molecules, let alone fragment-sized ones.<br /><br />This paper does demonstrate that it is possible to find fragments with lower affinities, though the weakest fragment with a reported dissociation constant comes in at 500 micromolar, and in that case the curve is not complete.<br /><br />Still, it is nice to see more people trying to advance fragments in the absence of structural information.Dan Erlansonhttps://www.blogger.com/profile/07927082337051189270noreply@blogger.com