It’s been two years since Practical Fragments updated its list of fragment-derived compounds in the clinic, and since then there have been some nice developments. The table below starts from the previous list and also includes everything new we've managed to find. As before, this includes compounds whether or not they are still in development (indeed, some of the companies no longer even exist). Drugs reported as still active in clinicaltrials.gov, company websites, or other sources are in bold, and those that have been discussed on Practical Fragments are hyperlinked to the most relevant post.
|Vemurafenib (PLX4032)||Plexxikon||B-Raf(V600E) inhibitor|
|ABT-199||Abbott||Selective Bcl-2 inhibitor|
|AT9283||Astex||Aurora, Janus kinase 2 inhibitor|
|Linifanib (ABT-869)||Abbott||VEGF & PDGFR inhibitor|
|Navitoclax (ABT-263)||Abbott||Bcl-2/Bcl-xL inhibitor|
|PLX3397||Plexxikon||FMS, KIT, and FLT-3-ITD inhibitor|
|ABT-518||Abbott||MMP-2 & 9 inhibitor|
|AT13148||Astex||AKT, p70S6K inhibitor|
|AZD5099||AstraZeneca||Bacterial topoisomerase II inhibitor|
The current list contains more than 30 clinical-stage drugs but is certainly incomplete, particularly in Phase I. If you know of any others (and can mention them) please leave a comment.