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

PDB Update

Posted by kinasepro on March 27, 2007

2GHG Abbott – Chk1 with A431994 (Akt inhibitor) BMCL ’06, 3424


I haven’t read the article yet, but to my eye the PDB suggests a ligand conformation responsible for some off target activity. Abbott’s indole-aminoethoxides in last weeks update (2OH0, 2OJF) seem to be the more typical (potent?) conformation.


2 Responses to “PDB Update”

  1. milkshake said

    just looking at the structure, this thing looks about as soluble as a piece of yellow-painted concrete (chipped from a speedbump)

  2. kinasepro said

    I got around to reading the bmcl… it underwhelmingly suggests they got the chk structure merely as a surrogate – that they couldn’t get a pkb, or pka mutant to crystallize. No mention of chk activity in the paper.


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