KinasePro

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

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

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4 Responses to “XL418”

  1. What do you think of these wrt PKA inhibition? Their pharmacophore looks a bit odd, especially when compared to Vertex/Abbott compounds which mostly incorporate a primary or secondary amine function in the ribose binding area?

    My sources tell me that Vertex AKT series was canned due to equipotent inhibition of PKA (their series was indazole based – not a million miles away from the pyrazolo-pyrimidines described here…..

    But then PKA only has around 120 target proteins if I remember correctly, so nothing to worry about with respect to toxic side effects!

  2. milkshake said

    I would worry more about a dramatic CYPs problem with this piece of work…

  3. weirdo said

    CYPs? Who cares, it’s a cancer drug . . .

  4. kinasepro said

    CYPs? Cancer? Combination Therapy?

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