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

Archive for November, 2006


Posted by kinasepro on November 30, 2006

Hey Hey Array, Chiral P38 inhibitors 4tw! It looks like this may be the ARRY-797 series. Let me first say this has got to be the most awesomest P38 presentation Kinasepro has ever seen. Thanks for hosting it, but I notice you don’t drop the structure for 797. Boo.


This is a provisional application, third in a series including: US2004192653, US2004180896, US2004176325. It appears to me that you guys tried to get away from the the chiral center in US2004192653, but it must be important as it looks like your back to hitting it hard with some asymmetric alkylations this app. (atypical in the kinase patentscape) And lastly for this doting review: the fluoro in the fluoro-isobutyl group is a nice touch.

Posted in Array, p38 | 3 Comments »

Giving thanks…

Posted by kinasepro on November 30, 2006

For finally getting my hands on last weeks list, so here it is in all its unfiltered glory:


I’ll report on what I can.. but with tomorrow’s coming fast, this may be a tough week.

Posted in Application List | Leave a Comment »

Kinase PDB’s: c-FMS

Posted by kinasepro on November 28, 2006

c-FMS (CSF1R if your from Cytopia.) is on the docket this week: 2IOV, 2IOY, 2I1M These are the first cFMS published methinks?

Well consider this colony stimulated.

Posted in c-fms, PDB | 1 Comment »

Monday night OT

Posted by kinasepro on November 28, 2006

Science Podcast Carnival v1.0

Nature and Science mags have podcasts. Check them out if you haven’t. No really – go now then come back later, I’ll still be here.

Science update is pretty cool, Nova has a couple and they are worth checking as well. Don’t forget the Popular Mechanics show <- More techy then sciency, but I still listen. Don’t forget the NYT Science times podcast.

But my personal favorite: Mysterious Universe

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Posted in Monday Night Off Topic | 1 Comment »

TPL2 4 Real?

Posted by kinasepro on November 27, 2006

Hey Wyeth, so is TPL2 for real? I see people have been talking up Cot/TPL2/MAP3K8 as another tnf-α inhibiting kinase target, but it seems that nobody else (cept maybe Abbott) seems to have jumped on board yet.

Yes that is a chloride atom there hugging the hinge.


Bioorg Med Chem Lett 2006, 6067
Bioorg Med Chem Lett 2005, 5288
(unrelated Abbott tpl2 series: WO2005110410)

ps. Thanks T.S. for the tip that wipo search feature bears much to be loved.

Posted in tpl2, Wyeth | 3 Comments »

BMS-354825 vs. VX-680

Posted by kinasepro on November 24, 2006

At least the PDB gave us something to look at a few days ago. Here’s a super-cool alignment of dasatinib in Abl to VX-680 in an abl mutant.

Posted in Aurora, bcr abl, BMS, Vertex | Leave a Comment »

World ‘o’ kinases takes the weekend off.

Posted by kinasepro on November 24, 2006

Not Kinasepro mind you, we’re here furiously searching for the latest and greatest in kinase related non-literature literature. It’s the rest of the world that seems to have taken this Thanksgiving weekend off. News agencies: nothing worth reporting. The USPTO: closed for the holiday so no thursday list. Its so bad that I’ve been forced to pour over a few German applications. No offense Merckle Biotech, but its a little hard to get excited about a couple p38 inhibitors that look like:

Posted in General Interest | Leave a Comment »

2 PDBs today

Posted by kinasepro on November 21, 2006

Today’s update to the PDB contains two interesting SRC / Abl inhibitors.

BMS’s dasatinib in Abl is 2GQG

Astra’s AZD0530 in SRC is 2H8H

Posted in Astra, bcr abl, BMS, PDB, SRC | Leave a Comment »

Quick Rundown

Posted by kinasepro on November 20, 2006

Paying homage to 1/2DPCB’s “Saturday Night Synthesis” with a little thematic post of my own. lets call it Monday night OT so here’s a little off topic ‘musing’. Feel free to tune out now. Else ->

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Posted in Monday Night Off Topic | 4 Comments »


Posted by kinasepro on November 20, 2006

Hey Hey J & J,  Nice c-FMS inhibitors.  As kinase inhibitors go these are new to me, but I see you’ve been banging away at these for a few years so there’s got to be a candidate in there somewhere, eh?

Posted in c-fms, J&J | Leave a Comment »