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

Archive for the ‘AKT’ Category


Posted by kinasepro on December 15, 2006

Hey Keryx, Good luck with the “Akt, MAPK, and JNK” Phase ii. Don’t’ know anything about the compound other then what you tell us: “KRX-0401 (perifosine) is in-licensed by Keryx from Aeterna Zentaris”

Might take a little digging to get at this one.


Posted in AKT, clinical, Jnk, p38 | 4 Comments »


Posted by kinasepro on December 1, 2006

Hidy Ho Merck and Co., I’d say nice AKT inhibitors, but I notice you’re doing your xeno studies sub-q.

Read the rest of this entry »

Posted in AKT, Merck & Co. | Leave a Comment »


Posted by kinasepro on October 31, 2006

Hi Again SKB, Nice AKT inhibitors.

This benzimidazole core keeps popping up in the patent literature… Maybe there’s something to it. I see you guys vary the heck out of the alkoxy-amino region. Some nice intermediates worth perusing there.

As for the binding motif, well, AKT appears to be difficult to crystallize, or else why would folks be looking at PKA mutants as PKB models? (1XH4, 1XH5, 1XH6, 1XH7, 1XH8, 1XH9, and 1XHA) KP is not aware of any PDBs with the core, and the two APO’s of akt are teh suq, but my feeling is that 2F7Z has some clues.

Yah, Yah I know the overlay is ‘backwards’ compared to the 2D models… Use your rimagination. This seems reasonable though and puts the oxadiazole at the hinge, the alkyne pointed towards H1, and the primary amine in the phosphate binding region. NC1=NON=C1C2=NC3=C(C#CC(C)(O)C)N=C(O[C@H]([C@H](COC)N)C4=CC=CC=C4)C=C3N2CC

Posted in AKT, GSK | 1 Comment »