KinasePro

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

Archive for the ‘AKT’ Category

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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.

Posted in AKT, Astex | 1 Comment »

MK-2206

Posted by kinasepro on April 23, 2009

Merck’s Ph1 allosteric AKT inhibitor:

NC1(CCC1)C(C=C2)=CC=C2C3=NC4=C(C=C3C5=CC=CC=C5)C(N6C=C4)=NNC6=OBinds 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 | 5 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It’s an AKT inhibitor, and its been Terminated & Withdrawn… Wonder why.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)OCancer Res, Blood, J Med Chem, Dartmouth?

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

Astrazeneca: CDK2 BMCL: 2W05

Amgen: P38 J Med Chem; 3DT1

LCK: 2ZM4, 2ZM1

Posted in AKT, CDK2, JAK, Lck, PDB, p38, 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

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.

Read the rest of this entry »

Posted in AKT, Abbott, 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

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

2GU8, AKT, Chiron, BMCL, 06, 4163

O=C(C1=CC=C(C2=NC(NC)=NC=C2)S1)N[C@@H](CC3=CC=C(Cl)C=C3Cl)CN

2OJ9, IGF-1R, BMS, BMCL, 07, 2317

O=C1C(C2=NC3=CC(N4C=CN=C4)=CC(C)=C3N2)=C(NCC5=NC=CC=C5)C=CN1

Posted in AKT, BMS, Chiron, IGF, PDB | 1 Comment »

XL418

Posted by kinasepro on January 31, 2007

IND in the books.

Looking something like: WO/2005/117909 WO/2006/071819

CC1=C(CCCN2CCCC2)C=C(Cl)C=C1N3CCN(C4=C5C(NN=C5Br)=NC=N4)CC3

Posted in AKT, Exelixis | 4 Comments »

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.

O=C(C1=CC=CS1)N(C2=NC(C3=COC4=CC=CC=C34)=CS2)CCCN5CCOCC5

>> 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 »

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