Practical Fragments

This blog is meant to allow Fragment-based Drug Design Practitioners to get together and discuss NON-CONFIDENTIAL issues regarding fragments.

Showing posts with label LE. Show all posts

Showing posts with label LE. Show all posts

08 July 2015

Merging Fragments for Matriptase

We often talk about methods here: how to screen, how to prosecute those actives, and everything in between. This is one of those what you ...

16 April 2014

What we do in life, echoes in eternity (or the life of the patent)

Next week is the Drug Discovery Chemistry conference where Dan and I will be co-teaching our award-winning FBDD short course (or at least...

12 February 2014

Fragments vs NAMPT, maximum ligand efficiencies, and off-target activities

The enzyme nicotinamide phosphoribosyltransferase (NAMPT) is essential for the synthesis of the important cofactor NAD and thus an intriguin...

03 February 2014

How weak is too weak for PPIs?

Ben Perry brought up an interesting question in a comment to a recent post about fragments that bind at a protein-protein interface: “At wh...

25 March 2013

Leave Them Asking for More

ret·ro·spec·tive (r t r -sp k t v) adj. 1. Looking back on, contemplating, or directed to the past. 2. Looking or directed backward...

11 March 2013

With the proper tool, I could move the world

As noted before , bromodomains are a "hot" area of drug discovery. Dan mentioned last year that PFI-1 was being released as a t...

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