KinasePro

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

Archive for September, 2008

You Need a Job

Posted by kinasepro on September 26, 2008

And KP wants to help.

Tell you what.  Upload your job talk somewhere, or better yet convert it to a shareable G-Doc, and KinasePro will get you exposure by linking to it.  If you want more details on how this can work – email me.

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Posted in Monday Night Off Topic | Leave a Comment »

AZD-7762

Posted by kinasepro on September 25, 2008

It’s going ph1, it’s from WO/2005/066163, and it’s been described.

O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@H]3CNCCC3

Somebody send it to AmbitXL-844PF-477736, IC-83 are the known competition.

Posted in Astra, Chk1 | Leave a Comment »

Takeda’s got…

Posted by kinasepro on September 24, 2008

a Jnk3 BMCL:

2ZDT and 2ZDU …reminds of 2R9S

Posted in Jnk, Takeda | Leave a Comment »

R & D @ B I

Posted by kinasepro on September 13, 2008

With BIRB-796 a distant memory, BIBW-2992 in ph3 and given the new name Tovok, BIBF-1120 headed into ph3 and given the name Vargatef,  BI-2536 in multiple Ph2s, a new Ph1 Aurora inhibitor, and another backup PLK1 inhibitor undisclosed, but likely in-clinic or clinic-bound – what could possibly be next?

I can haz pyrimidines

PDK mod prolly from Berlex

Posted in BI, PDK1, PKC, Plk1 | 2 Comments »

Eck’s Got FAK

Posted by kinasepro on September 9, 2008

2JKQ, 2JKK, 2JKO, 2JKM,

Neat helix, & 2JKK is NVP TAE-226 but 2JKM (non-helix) is the closest thing to anything FAK in the clinic: PF-562271

Posted in FAK | Leave a Comment »

Jnk Science

Posted by kinasepro on September 9, 2008

Roche Palo Alto just published 3E7O: JNK2 (7x mutant) bound to an indazole:

Which brings up that nearly two years ago I suggested CC-401 may be from an ’06 Celgene application.  Right flavor wrong compound, the drawn compound is CG-930 (IND filed Dec 18, 2007 – claimed in Ph1 for fibrotic diseases).  As NCI suggests CC-401 is an SP-600125 analog which incidentally is no longer on the CG pipeline.   C12=C(C=C(C=C2)C3=NN=CN3)C(C4=CC(OCCN5CCCCC5)=CC=C4)=NN1

That’s life on the edge for yah.

Posted in Celgene, Jnk, Roche | Leave a Comment »

PF-3814735

Posted by kinasepro on September 5, 2008

It’s Pfizer’s Ph1 Aurora inhibitor:

O=C(N1[C@H]2C3=CC=C(C=C3[C@@H]1CC2)NC4=NC(NC5CCC5)=C(C=N4)C(F)(F)F)CNC(C)=O

Posted in Aurora, Pfizer | Leave a Comment »

Who cares about the Roche p38 inhibitors?

Posted by kinasepro on September 5, 2008

Probably a few less people in PA then a few months ago, eh?  But this one’s been getting press recently:

CN(C(C(N1CCCCC1)=NN2)=C2C=C3C4=CC(C(NC)=O)=CC=C4C)C3=O

WO/2008/104473

Posted in p38, Roche | Leave a Comment »

Best of KP

Posted by kinasepro on September 5, 2008

In case you came late to the party, here’s some of my favorites:

The Kinaverse

Approved Kinase Inhibitors

Ph3 Kinase inhibitors

S—-O

Cl—-O

Note the RSS feed of my reading list.

Also note comments are closed – email me if you’ve got something to say, or start your own blog.  Go on – Its fun.

Posted in General Interest | Leave a Comment »

AZ’s Bis-Morpholine

Posted by kinasepro on September 4, 2008

+ XRPD on multiple salt forms of this EphB4 inhibitor:

OCC1=CC=C(C)C(N(C2=NC(NC3=CC(N4CCOCC4)=CC(N5CCOCC5)=C3)=NC=C2)C)=C1

WO/2008/104754

Posted in Astra, EphB4 | Leave a Comment »