KinasePro

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

Archive for August, 2008

GSK-690693

Posted by kinasepro on August 23, 2008

GSK’s AKT Alkynes?

Yah, you heard it here first. So Technically these are at least 3 years behind the times…

NC1=NON=C1C(N2CC)=NC3=C2C(OC[C@@H]4CNCCC4)=CN=C3C#CC(C)(C)O

neener.

Posted in AKT, GSK | Leave a Comment »

Ceph ‘n’ PCOP got C-Met

Posted by kinasepro on August 21, 2008

The 15M Pharmacopeia and Cephalon deal from a couple years ago was likely for compounds like these c-Met / Alk inhibitors:

O=C(NC)C1=CC=CC(F)=C1NC2=NC(NC3=CC=C4C(C)(C)CC(NCCOC)CNC4=C3)=NC=C2Cl

O=C(NC)C1=CC=CC(F)=C1NC2=NC(NC3=CC=C4C(C)(C)CC(NCCOC)CNC4=C3)=NC=C2Cl

WO/2008/051547

yeh, its 1300 pages and I know they’re old, but I got some catching up to do…

Posted in c-Met, Cephalon, Pharmacopeia | Leave a Comment »

At least its free…

Posted by kinasepro on August 20, 2008

The new ‘Perspective‘: Some useful information bracketed by useless commentary.

Affinity is not even a check-box on the road to an approved drug.  What’s stopping 99.9% of real compounds coming from real programs isn’t potency.  This makes a discussion of how many hydrogen bonds to the hinge are in approved drugs totally irrelevant.

Fact Check:

>> Ruboxistaurin is not an approved drug.

>> Fasudil is only approved in Japan.

>> And you forgot Tasigna

Posted in Cephalon, General Interest | Leave a Comment »