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

Archive for the ‘Rho’ Category

Some highlights…

Posted by kinasepro on November 28, 2007

GSK’s been looking at Plk1 for quite a while. Sure the structure was in an earlier application (March), but here it is better late then never. See: WO/2004/074244, WO/2004/087652, WO/2005/019193, WO/2007/030361, US20070010668, & US20070270437

AP-24534 In here? Earlier Ariad had a double bond wiggling around T315I, in WO/2007/133560 & WO/2007/133562 it’s a triple bond.

And Vertex has an interesting series of series of Rock inhibitors in WO/2007/133622. Ki is reported to be <100 nM and clean across the cyps.

Oh yah, and if your curious about Cyclacel’s Aurora inhibitor CYC-116, they’ve narrowed it down to 1 of 3 for you and they also give an in vitro panel in WO/2007/132220, WO/2007/132221, WO/2007/132228. The claims make it look like the morpholine.

Posted in Ariad, bcr abl, Cyclacel, GSK, Plk1, Rho, Vertex | 4 Comments »

Astellas ‘n’ Rock1

Posted by kinasepro on March 14, 2007


via WO/2007/026920

Posted in Astellas, Rho | Comments Off on Astellas ‘n’ Rock1

Swing Rho,

Posted by kinasepro on December 5, 2006

Sweet Chariot… Ehhem, umm, uhh, pardon me, pardon me, though its not unlike Kinasepro to break into song in the presence of greatness, so perhaps you’ll grant me this.

The PDB has been hot lately, this week its Part two in a Rho series with Y27632 (a ROCK inhibitor) bound to Rho: 2H9V.

 2FSU was the first Rho xray published via the same group earlier this year. Also of note, 2GNJ tried to model Rho with a 5-fold mutant of PKA bound to this same inhibitor. By the looks of this one, they got it pretty close.

There’s also a string of p38 mutants: 2FSL, 2FSM, 2FSO, 2FST,

Posted in PDB, Rho | Leave a Comment »