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


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

6 Responses to “MK-2206”

  1. milkshake said

    OMG: 1-subst cyclobutyl amine sidechain. The Merck management is full of imbecile twits but they still get the best synthetic chemists

  2. G2 said

    Shouldn`t it be a 2H-[1,2,4]Triazolo[3,4-f][1,6]naphthyridin-3-one core?

  3. kinasepro said

    Thanks, I believe your correct. Revised structure should show now. & Here’s a scheme for you synthesis junkies.

  4. Warren said

    Merck has been working on compounds like this for a long time.
    Mol Cancer Ther 2005;4(2).
    Did they ever show whether compounds in this series bind to other PH domains in other proteins?

  5. Nutrivie said

    Are there any PI3K inhibitors available for research that are known to specifically and ONLY inhbit P110a?

  6. JT said

    Is this soluble in DMSO?

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