KinasePro

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

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?

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