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


Posted by kinasepro on January 2, 2010


Posted in General Interest | 6 Comments »


Posted by kinasepro on September 1, 2009

This PDB entry confirms the structure.


as always, being 18 months behind the times put you 6 months ahead of the curve.

Posted in MEK | 3 Comments »

p38: Not dead?

Posted by kinasepro on August 13, 2009

Well.. maybe this compound will kill it: Polymorphic Forms / WO/2009/098612 & its from Pfizer no less –


Part Axitinib, part Birb, Part SGX… All MW: 700

Thanks for the email PN.

Posted in p38, Pfizer | 8 Comments »


Posted by kinasepro on August 7, 2009

Astex has released data about their AKT program, including a PDB, but I have omitted that they appear to have dropped the strutcture of their candidate in WO/2008/110846


Thanks, Ed.

Posted in AKT, Astex | 1 Comment »


Posted by kinasepro on August 1, 2009

A comments to BMS-777607 suggest that this structure is the backup:



Posted in BMS, c-Met | 6 Comments »


Posted by kinasepro on July 31, 2009

Its a salt form of ENMD-981693…CC1=CC(NC2=NC(/C=C/C3=CC=CC=C3)=NC(N4CCN(CC4)C)=C2)=NN1

Posted in Aurora | 3 Comments »

AZ’s got PI3K

Posted by kinasepro on July 30, 2009


WO/2009/093972 reminds you of…

Posted in Astra, pi3k | 3 Comments »

Pi3k @ Bayer

Posted by kinasepro on July 25, 2009

This one hones in on the sulphonamides: (from the former site in CT)O=C(C1=CC=CN=C1)NC2=NC3=C(OC)C(OCCOCCNS(C)(=O)=O)=CC=C3C4=NCCN24

WO/2009/091550; They stuck morpholines out there previously: WO/2008/070150

Posted in Bayer, pi3k | 1 Comment »

Biogen Nominated…

Posted by kinasepro on July 14, 2009

… A RAF candidate & Sunesis got a milestone,

In August 2004 the companies entered into a collaboration to discover and develop small molecule cancer therapeutics targeting kinases, a family of cell signaling enzymes that play a major role in the progression of cancer. The research term of this collaboration ended in June of 2008. Sunesis retains an option to participate in the co-development and co-promotion of the Raf kinase inhibitor resulting from this collaboration.

Likely derived from WO/2009/006389WO/2009/006404


Posted in Biogen, RAF, Sunesis | 2 Comments »

What do…

Posted by kinasepro on July 10, 2009

…the Bee Gee’s and R406 have in common?

R-788 (a prodrug of R-406) has shown promise in a Ph2b trial. Partner Plz?

riglstill no BMCL

Posted in Rigel, SYK | 2 Comments »