KinasePro

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

Archive for the ‘Astex’ Category

AT-131418

Posted by kinasepro on August 7, 2009

Astex has released data about their AKT program, including a PDB, but I have omitted that they appear to have dropped the strutcture of their candidate in WO/2008/110846

O[C@](CN)(C1=CC=C(Cl)C=C1)C(C=C2)=CC=C2C3=CNN=C3

Thanks, Ed.

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Posted in AKT, Astex | 1 Comment »

AT-9283

Posted by kinasepro on March 18, 2009

Astex’s unpartnered JAK/Aur/Abl Ph1b nibO=C(NC1=CNN=C1C2=NC3=C(N2)C=CC(CN4CCOCC4)=C3)NC5CC5

poster; clinic; PDB: 2W1G & 2W1I

Posted in Astex, Aurora, bcr abl, JAK | Leave a Comment »

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 »