KinasePro

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

CX-4945

Posted by kinasepro on April 19, 2009

Cylene’s CK2-α selective inhibitor currently in Ph1:

OC(C1=CC2=C(C3=CN=CC=C3C(NC4=CC=CC(Cl)=C4)=N2)C=C1)=O

Ki 0.38 nM

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9 Responses to “CX-4945”

  1. bioanalytik said

    I don’t know where you got this IC50 from, but my Informations were 2 nM against recombinant CK2 and 100 nM in Jurkat…

  2. weirdo said

    Hey, it’s a kinase IC50, you can get whatever IC50 you with a little effort . . . .

  3. kinasepro said

    That’s probably the Kd, and I unfortunately don’t have more info

  4. jacko said

    Wow, how did a compound like this make it through profiling? Unsubstituted aniline, carboxylic acid, and possible DNA intercalator. Hmmmm……

    • kinasepro said

      Some folks are umm… less ‘inhibited’ by functional group phobias.

      This aniline can’t really form a nitroso-amine so I’m not worried about that (see p 683)… The acid likely contributes to protein binding which the backup likely isosteres out.

  5. viledonkey said

    Yep, I’d also be surprised if that anilino function undergoes nitroso formation – the heterocycle is too electron poor (c.f. tarceva, iressa, etc….) More surprised that this is an oral therapy……love to know the Cmax.

    Am also impressed how acidophilic CK2 is……..

  6. Warren said

    Of course casein kinases like acids, they like casein–a big old anion (isoelectric point is about 4.5)

  7. bioanalytik said

    Hey KinasePro. Structure is wrong! Where did you get it from? The real CX-4945 is Cl-substituted !

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