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

Raf… Weird…

Posted by kinasepro on September 23, 2007

Wyeth’s got some new RAF stuff with US20070219186:


data on p19

This one’s got me wondering…


7 Responses to “Raf… Weird…”

  1. Murray said

    …interesting…hinge interaction not required for RAF potency. Selectivity…

  2. kinasepro said

    Yah, and it has me taking a re-look at the recent Novartis app.

  3. xtallographer said

    well, *raf* is weird…..

  4. binding said

    Are we sure that it doesn’t bind to the hinge?

  5. kinasepro said

    My guess is the pyrimidyl N tags an H20 which in turn hits the hinge. So… yes and no.

  6. Mastan said

    Example 312 is not the compound above. Are you thinking about a different one, perhaps?

    [0312] ethyl 7-(3-{[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)carbonyl]amino}phenyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate

  7. kinasepro said

    Thanks for the correction, there goes that dyslexia again… its example 315 which has now been modified above. – The IC50 did match the structure however. (also note that ctrl-F on “example 315” is differn’t then [0315] and likewise for [0312])

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