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


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 »

Aurigene’s Insights

Posted by kinasepro on May 29, 2009

A Big thanks to Aurigene‘s [colorblind] scientists who have been gracious enough to share with us this presentation given in India at a recent med-chem conference.

aurigeneStructural Insights into Kinase Inhibition
More like this please!

Posted in General Interest | Leave a Comment »

Allosterism: A Diatribe

Posted by kinasepro on May 25, 2009

So just what is an allosteric kinase inhibitor?

Read the rest of this entry »

Posted in General Interest, gleevec | 8 Comments »

BAY 73-4506

Posted by kinasepro on May 20, 2009

So Bayer is in Ph2 with fluoro-sorafenib aka DAST, BAY-734506… Only this time they’re in without Onyx and I gather Onyx is none too happy about this.

BAY-734506The distinct compound is claimed in WO/2005/009961 and the I believe the original Sorafenib app is: WO/2000/042012.  What strikes the chemist inventor about a structure like this isn’t usually about who owns it, but if it can really be considered a new invention? The claim structure in the 2000 Sorafenib application can be schematized:

sorafenib-claimsSo for the purpose of this discussion the only meaningful definition is the ring designated as “L” and whether or not they claim the fluoride:

L-definedAnyhow while this structure and their priority date may be vulnerable to obviousness, all of these applications are assigned to Bayer, and not Onyx, so that disagreement will more likely be resolved based on the wording of the Onyx / Bayer contract.  The Onyx press release suggests this very structure was discovered during the collaboration…  We’ll see.  Given the timing I bet someone saw the structure here on Kinasepro and told Onyx, heh.

Posted in Bayer, RAF, VEGF | 5 Comments »


Posted by kinasepro on May 18, 2009



an A-loop doesn’t do that! (its new SGC prerelease of  a BI-PLK1-like inhibitor bound to TTK)

Posted in PDB, SGC | Leave a Comment »