Archive for the ‘pim1’ Category
Posted by kinasepro on May 3, 2009
Posted by kinasepro on October 22, 2008
Posted by kinasepro on September 4, 2008
WO/2008/106692 is Novartis’ Emeryville’s Pim1,2,3 < 1uM offering:
Posted by kinasepro on April 11, 2007
>> update: Amanda‘s already on the scene… and fascinated.
2OI4’s ‘nother one of them CP-Ruthenium/Stuarosporine things bound to PIM1
Posted by kinasepro on February 8, 2007
Maybe this why they call it pim1?
See here, its a kinase without a key hydrogen bond donor. Highlit yellow is the interesting PRO123. ATP and inhibitors generally bind to the peptide NH that is otherwise normally there.
Big deal eh? Well, next time a modeler tells you you have to have a hydrogen bond to the hinge, tell him to put 2OBJ in his pipe and smoke it! 1YI3 is the other ligand/pim complex. While I don’t know the activity of these pyridone compounds or of the ligand in 1YI3, BindingDB has 5 compounds 4 of which are 150nM and less. SS and the BIM’s appear to be very active. I guess when your competition is ATP, and ATP can’t find that H-Bond either…
Previous PIM1 PDB’s: 1XQZ, 1XR1, 1XWS, 1YHS, 1YI3, 1YI4, 2BIK, 2BIL, 2BZH, 2BZI, 2BZJ, 2BZK, 2C3I, 2OBJ