KinasePro

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

Archive for October, 2008

Boo!

Posted by kinasepro on October 31, 2008

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Posted in General Interest | Leave a Comment »

PDB Update

Posted by kinasepro on October 29, 2008

Aurora A + 680: 3E5A; Protien Sci

Aurora B: 2VGO; Mol Cell Ther

SRC: 3EL7 & 3EL8; Chem Biol;

EPHB4: 2VWX; 2VWY; 2VX0, 2VX1

Posted in Aurora, EphB4, PDB, SRC | 2 Comments »

CH——-Pi

Posted by kinasepro on October 23, 2008

Kissei’s done a little math on LCK ligands and suggests the stablization owes to those methyl’s.

BMCL

Cool, yah ,so, umm, like, thats why they gotta be flat.

Posted in General Interest, Lck | 8 Comments »

ARRY-704 ?

Posted by kinasepro on October 23, 2008

aka ARRY-424704 / AZD-8330 is the Array / Astra Mek Ph1 backup to ARRY-886 / AZD-6244 which was put in a holding pattern when it didn’t meet a ph2 endpoint. The pictured strucuture is ‘Mek Inhibitor II’ in the combination app WO/2008/125820:O=C(C(C=C1C)=C(NC2=CC=C(I)C=C2F)N(C)C1=O)NOCCO

Posted in Array, Astra, MEK | 2 Comments »

Wyeth’s IKK candidate

Posted by kinasepro on October 23, 2008

US20080262010: D-glucuronate
US20080262009: acetate
US20080262008: succinate

Posted in IKK, Wyeth | Leave a Comment »

WO/2008/124161

Posted by kinasepro on October 22, 2008

Exel’s got Pi3K-a in combination: Reminds one of the XL-147 combo study.

COC1=CC2=C(NC3=CC=C(Cl)C(Cl)=C3F)N=CN=C2C=C1OCC(C4)C[C@]5([H])[C@@]4([H])CN(C)C5

So thats XL-647 ?  I hadn’t heard.

Posted in EGF, Exelixis, pi3k | Leave a Comment »

WO/2008/124323

Posted by kinasepro on October 22, 2008

Array’s got Pim:

F[C@H]1CNCC[C@@H]1OC2=CC=CC(C2=N3)=CC=C3C4=CN=C5N4C=CC(OC6CCOCC6)=C5

Posted in Array, pim1 | Leave a Comment »

US20080255162

Posted by kinasepro on October 22, 2008

Pfizer’s got PI3K:

O=C(C1=CC(NC2=NC(C)=C(C=CC(N3C4CCCCC4)=O)C3=N2)=CN1C)O

previously:

Posted in Pfizer, pi3k | Leave a Comment »

SGC’s got…

Posted by kinasepro on October 17, 2008

Lots ‘o’ new stuff

DYRK1A: 2VX3


Haspin: 3E7V, 2VUW, 3DLZ

v-FES + SS: 3CD3,3CBL,3BKB; CELL

Posted in PDB, SGC | Leave a Comment »

UCB’s got a chart

Posted by kinasepro on October 15, 2008

go check it out.

Posted in clinical, General Interest | Leave a Comment »