KinasePro

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

Archive for the ‘CDK’ Category

Roscotivine: The Saga

Posted by kinasepro on May 13, 2009

mmm KinaseBlogging:

Part 1, 2, 3, & 4

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Posted in CDK | Leave a Comment »

SCH-727965

Posted by kinasepro on March 27, 2009

Schering-Plough’s CDK1,2,5,9 inhibitor in Ph2 for lung cancer:

O=N1=CC=CC(CNC2=CC(N3CCCC[C@H]3CCO)=NC4=C(CC)C=NN42)=C1

WO/2009/038701 has quite a bit to say about the clinical protocol including human PK and a very clean dose response measuring BrdU incorporation.

Posted in CDK, Schering-Plough | 5 Comments »

Postcards from Vienna…

Posted by kinasepro on October 1, 2008

Hey look what I got:

Yah, its the disclosure of the discovery of PHA-848125.  Not only that, its a pretty good poster. This also means I was wrong again!

Posted in CDK, Nerviano | 7 Comments »

Astex: An Oral Candidate for CDK2

Posted by kinasepro on November 23, 2007

Astex’s fragment based discovery effort yielded an oral candidate back in ’05, and now with WO/2007/129066 & WO/2007/129062 the world can have a look. It’s probably AT-9311 even though I could’a swore I heard’m say that their Novartis’ partnered material was of a different series then AT-7519. Perhaps its 7519 I have wrong…

O=C(C2=NNC=C2NC(C3=C(Cl)C=CC=C3Cl)=O)NC1CCN(S(=O)(C)=O)CC1.O=C(C5=NNC=C5NC(C6=C(Cl)C=CC=C6Cl)=O)NC4CCNCC4.N7=CC=CN7

pM CDK2
0.22 uM GSK3b
Mouse: 40-50%F (DMSO/Water/PEG 1/2/7)

Posted in Astex, CDK, CDK2 | 12 Comments »

Nerviano ‘n CDK

Posted by kinasepro on August 19, 2007

>> Update >> its really PHA-848125

WO/2007/90794 is a CDK inhibitor in combination with yada yada… from Nerviano.  The single compound claimed is pictured and potentially the phase one compound: PHA-793887.

O=C(C1=NN(C)C2=C1C(C)(C)CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=C4)N=C23)NC

Discovery: Pharmacia IT WO/2004/104007

Posted in CDK, Nerviano | 4 Comments »

/. does CDK5

Posted by kinasepro on July 16, 2007

For my read, the story is less that MIT CURES PHEAR! and more that, heh – slashdot picked up a kinase related press release – then proceeded to mangle it. 😦 Nobody tell Derek.

In our study, we employ mice to show that extinction of learned fear depends on counteracting components of a molecular pathway involving the protein kinase Cdk5

MIT Press release; Nature Neuroscience; Falculty page

Posted in CDK, General Interest | 4 Comments »