Kinase Chemistry – Just a year and a half behind the times.

Archive for March, 2009


Posted by kinasepro on March 28, 2009

Incyte’s Ph2 Jak 1, 2 inhibitor: Org Lett; see also: WO/2008/157208


Keeping pace with CP-690550

Posted in JAK | 9 Comments »

The History of Gleevec

Posted by kinasepro on March 28, 2009

chemistry @ 22:30

It’d be great if someone were to crystallize the first hit with Abl or Kit and compare this with 1IEP.  I suspect this would put the paradigm of structure based design in perspective.

Posted in gleevec | Leave a Comment »


Posted by kinasepro on March 27, 2009

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:


WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

Posted in CDK, Schering-Plough | 5 Comments »


Posted by kinasepro on March 26, 2009

BMS homegrown Ph1 c-Met / AXL / Ron Inhibitor.  As of now PDB 3F82 has not yet been released.


The N-Oxide is a major metabolite, and from the trial notes its either toxic, potent, or prevalent… The J Med Chem doesn’t mention it.

Posted in BMS, c-Met | 1 Comment »


Posted by kinasepro on March 26, 2009

Is the screening company’s Ph1 FLT-3 compound:


polymorph app: WO/2009/038757

Posted in Ambit, Flt3 | Leave a Comment »


Posted by kinasepro on March 24, 2009

Structure’s a guess from process app: WO/2009/031011


Posted in Pfizer, Rigel, SYK | 2 Comments »


Posted by kinasepro on March 24, 2009

Eisai’s Ph1 VEGF inhibitor


Posted in Eisai, VEGF | Leave a Comment »


Posted by kinasepro on March 23, 2009

Aveo’s Vegf inhibitor; currently Ph ii in RCC & NSCLC;


Formerly KRN-951 & pM against 1, 2, & 3

Posted in VEGF | 5 Comments »

GSK’s got C-Met

Posted by kinasepro on March 19, 2009

WO/2008/049855 bears a certain resemblance to XL-184.


btw: XL-880 is now going by GSK-1363089

Posted in biotech, c-Met, GSK | Leave a Comment »


Posted by kinasepro on March 18, 2009

Here’s one where they do tell us why its off the pipeline:


J Med Chem -> Chem Res Tox

Read the rest of this entry »

Posted in Amgen, c-Met | Leave a Comment »