KinasePro

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

Archive for December 12th, 2006

VX-680

Posted by kinasepro on December 12, 2006

Oh wait I’m sorry Merck. My bad, I didn’t realize we’re calling it MK-0457 now. heh… Phase 1 update presented yesterday. The compound hits Aurora, JAK2, Abl etc. etc. and the current study is in ph1 for colorectal cancer. Looks good.

We’ve talked about the compound before here.

Posted in Aurora, clinical, Merck & Co., Vertex | Leave a Comment »

PDB Update

Posted by kinasepro on December 12, 2006

The highlight is GSK’s SB-590885 bound to B-Raf: 2FB8 (They describe the oxime as a phenol isostere)

O\N=C1CCC2=C/1C=CC(C(N=C(C3=CC=C(OCCN(C)C)C=C3)N4)=C4C5=CC=NC=C5)=C2

Also, Amgen released the structurally interesting IRAK-4 bound to staurosporine (2NRY), and a benzimidazole inhibitor (2NRU). The Bioorg Med Chem Lett came out in March and the Xray is featured in this Structure paper.

CC(C)(C)C(OC1=CC=C2C(N=C(NC(C3=CC=CC([N+]([O-])=O)=C3)=O)N2CCCO)=C1)=O

The tyrosine gatekeeper is certainly different

Looks like there’s an indolinone lodged in today’s update as well. 2JAV replaces 2CL1, dunno why, probably some sort of refinement. NEK2 ne1?

Posted in Amgen, GSK, IRAK, PDB, RAF | Leave a Comment »

Monday night OT

Posted by kinasepro on December 12, 2006

Being an arrogant prick most of the time means sometimes haveing to say your sorry…

Read the rest of this entry »

Posted in Monday Night Off Topic | Leave a Comment »