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
(C1=CC=C(Cl)C=C1)C(C=C2)=CC=C2C3=CNN=C3](https://kinasepro.wordpress.com/wp-content/uploads/2009/08/at-131418.jpg "AT-131418")
Thanks, Ed.
Archive for the ‘AKT’ Category
MK-2206
Posted by kinasepro on April 23, 2009
Merck‘s Ph1 allosteric AKT inhibitor:
Binds to the Pleckstrin homology domain
@
Akt1 8 nM
Akt2 12 nM
Akt3 65 nM
thanks Ghost and Redferret for the structure
Posted in AKT, Merck | 6 Comments »
Gsk-690693
Posted by kinasepro on March 18, 2009
It’s an AKT inhibitor, and its been Terminated & Withdrawn… Wonder why.
![CC(C)(C#CC1=NC=C(C2=C1N=C(N2CC)C3=NON=C3N)OC[C@@H]4CNCCC4)O](https://kinasepro.wordpress.com/wp-content/uploads/2009/03/gsk690693.jpg?w=350&h=283 "gsk690693")
Posted in AKT, GSK | 3 Comments »
Plethora ‘o’ PDB’s
Posted by kinasepro on October 14, 2008
GSK’s AKT stuff: 3d0e, 3E8D, 3E87, 3E88; J Med Chem, KP
SGX: Jak2 3E64, 3E63, 3E62, BMCL
Shokat: SRC, SRC, SRC, SRC, PI3K-Gamma, PI3K-Gamma
reminds me of OSI-906 or vice versa
Amgen: P38 J Med Chem; 3DT1
Posted in AKT, CDK2, JAK, Lck, p38, PDB, pi3k | Leave a Comment »
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](https://kinasepro.wordpress.com/wp-content/uploads/2008/08/gsk-akt1.jpg?w=220&h=172)
neener.
Posted in AKT, GSK | Leave a Comment »
PDB Update
Posted by kinasepro on June 5, 2007
Some kind of coincidence that this week’s update are all indazoles? Hmm…
2UZT Abbott; AKT;
2UZU A-443654
2UZV
2UZW
The real action with these is what’s going on with the indole though.
Posted in Abbott, AKT, PDB | Leave a Comment »
VQD-002
Posted by kinasepro on May 2, 2007
Vioquest recently gave an update on their ph i/iia study with this here nucleotide. Nearly as old as ATP itself, the compound was made new again by a diagnostic screen for cancers overexpressing AKT.
![NC1=NN(C)C2=C3C(N([C@H]4[C@@H]([C@@H]([C@@H](COP(O)(O)=O)O4)O)O)C=C13)=NC=N2](https://i0.wp.com/img412.imageshack.us/img412/5434/triciribinebc5.jpg)
Also goes by: API-2, NSC-154020, TCN-P, and triciribine phosphate. and yeh, somebody got the structure wrong in Cancer Res. 04, 4394
(KSR v. Teleflex? suck it.)
Posted in AKT, biotech | Leave a Comment »
PDB Update
Posted by kinasepro on May 1, 2007
C=C3Cl)CN](https://i0.wp.com/img127.imageshack.us/img127/1739/aktks2.jpg)
DNA WEEK
Posted by kinasepro on January 11, 2007
Helluva week for Genentech
1) Partners up XL518
2) Makes Fortune’s #2
3) Boasts at JP Morgan: ‘We’ve got too much money’
4) Loses a Supreme Court decision vs. Medimmune
5) Submits year end 8k
6) Buys Amphora’s “unnamed” (AKT) program.
…Genentech will purchase Amphora’s entire program for an unnamed oncology target with the potential to treat multiple oncology indications. Other terms of the agreement were not disclosed.
Not partner mind you: purchase. Amphora’s most recent AKT application is WO/2006/020767. Chiron appears to have the closest AKT examples in WO/2005/095386 included for the helluvit.
>> UPDATE 5/1/07 >> Genentech is now listed as an applicant the Amphora application: WO/2006/020767. Other Amphora ‘ATP-Utilizing Enzyme Inhibitors: ‘WO/2005/033102 & WO/2005/097758 (same inventors)
Posted in AKT, Genentech | 2 Comments »
KinasePro 
