KinasePro

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

Archive for the ‘pim1’ Category

SGI-1776

Posted by kinasepro on May 3, 2009

Supergen’s Pim kinase inhibitor via WO/2008/58126: Structure described at AACR.

sgi-1776(keep’m coming please I know there’s more!)

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WO/2008/124323

Posted by kinasepro on October 22, 2008

Array’s got Pim:

F[C@H]1CNCC[C@@H]1OC2=CC=CC(C2=N3)=CC=C3C4=CN=C5N4C=CC(OC6CCOCC6)=C5

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Chiron’s got Pim

Posted by kinasepro on September 4, 2008

WO/2008/106692 is Novartis’ Emeryville’s Pim1,2,3 < 1uM offering:

O=C(C1=C(N)C=CC(C2=CC(C(N(C)C)=O)=CC=C2F)=N1)NC3=C(N4C[C@@H](N)CCC4)C=CN=C3

Posted in Novartis, pim1 | 2 Comments »

PDB Update

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

related: 2BZH, 2BZI, 2BZJ

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Partially Immitation Uno

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.

O=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1

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

Posted in pim1 | 1 Comment »