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Archive for the ‘CK2’ Category

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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Posted in CK2 | 9 Comments »

PDB Update

Posted by kinasepro on November 6, 2007

c-Met + Indolinone: 2RFS; Amgen
c-Met + pyrimidone: 2RFN; Amgen <- Clearly the highlight of the day, but no image from me yet. I’m looking at it wondering where did all the polar contacts go? Peculiar structure, but noteworthy as the first published structure in the xl-880/kirin/bms/genentech/array/methylgene acyl urea isostere genre.

CDK2 + a pyrimidine macrocycle: 2J9M; chemmedchem; Schering AG

CK2: 2RKP: 1.56A

PKA: 2QCS

Posted in c-Met, CDK2, CK2, PDB | 5 Comments »

EXEL & CK2

Posted by kinasepro on April 30, 2007

And then theres those 3 applications on CK2 from Exelixis WO/2007/048064, WO/2007/048065, & WO/2007/048066… The latter two with and / or Pim1 & 2 inhibition.

O=C1C=C(C2=CC(C)=C(O)C=C2)C=C(C3=CC=C(C(NCCN(CC)CC)=O)C=C3)N1

Seems plausible that CK2 could be one of the ‘undisclosed’ targets of the BMS collaboration.

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