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

Archive for June, 2009


Posted by kinasepro on June 28, 2009

It’s a Ph1 Aurora A/B/C inhibitor for ‘solid tumors’.  Seems likely to be a member of one of the phthalazine series’ WO/2008/124083, WO/2008/057280, WO/2007/100646, or WO/2007/087276.


Posted in Amgen, Aurora | 2 Comments »


Posted by kinasepro on June 18, 2009

TAK-901 is Takeda’s ph1 Aurora B kinase inhibitor & US20090156557 suggests its:O=C(C1=C(C)C2=C(C(C3=CC=CC(S(=O)(CC)=O)=C3)=C1)C4=CC(C)=CN=C4N2)NC5CCN(C)CC5


Posted in Aurora, Takeda | 7 Comments »


Posted by kinasepro on June 9, 2009

In Ph2 for COPD & it’s an atropisomer…(biochem)


Who wants to guess if its R or S

Process App: 20080177077
Backup: 20080269264

Posted in p38, Pfizer | 6 Comments »

Off Targets

Posted by kinasepro on June 9, 2009

Just when you thought this stuff was easy… Turns out:

* Gleevec & Nilotinib hit ‘α-carbonic anhydrase‘ (wiki). (not to mention p38ß)

* Sorafenib hits P38 (new structure),

* GW-5074 (cRaf inhibitor) weakly hits glutamate dehydrogenase (~2uM, new structure, wiki).

Posted in General Interest | Leave a Comment »


Posted by kinasepro on June 3, 2009

aka Palladia, PHA-291639, & SU11654 got its FDA Approval today! Well… In dogs at least:.  It’s for canine mast cell tumors.

O=C(NCCN1CCCC1)C2=C(NC(/C=C3C(NC4=C\3C=C(C=C4)F)=O)=C2C)C yeh, its the pyrrolidine version of Sutent & its the phosphate salt

Posted in Approved, Pfizer | 8 Comments »


Posted by kinasepro on June 2, 2009

Two allosteric inhibitors are better then one!

AZD-6244 is Array’s MEK inhibitor [ARRY-886] which failed a solo ph2 endpoint not too long ago.

MK-2206 is Merck’s ph1 AKT inhibitor

Posted in Array, Astra, Merck & Co. | Leave a Comment »