B-Raf - Furans- GSK

The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. Takle AK, Bamford MJ, Davies S, Davis RP, Dean DK, Gaiba A, Irving EA, King FD, Naylor A, Parr CA, Ray AM, Reith AD, Smith BB, Staton PC, Steadman JG, Stean TO, Wilson DM.

PDK1 Modeling - University of Kentucky

Combined 3D-QSAR Modeling and Molecular Docking Study on Indolinone Derivatives as Inhibitors of 3-Phosphoinositide-Dependent Protein Kinase-1. Abdulhameed MD, Hamza A, Liu J, Zhan CG.

Selectivity Prediction - Pfizer

Predicting Kinase Selectivity Profiles Using Free-Wilson QSAR Analysis. Sciabola S, Stanton RV, Wittkopp S, Wildman S, Moshinsky D, Potluri S, Xi H.

Patent Applications - 08/22/2008

US20080200496
SUBSTITUTED 1H-PYRROLO[3,2-b, 3,2-c, and 2,3-c]PYRIDINE-2-CARBOXAMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE Ie The present invention discloses and claims compounds of formula (I) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective...

US20080200486
Combination Of Organic Compounds The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) an mTOR kinase inhibitor and a method for treating or preventing a...

US20080200485
Kinase Inhibitors Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase....

US20080199426
Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders Disclosed herein are methods for treating a vascular inflammatory disorder or endothelial cell disorder using inhibitor compounds that inhibit the expression or biological activity of Tie-1, Tie-1...

US20080200509
3,4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASE AND GLYCOGEN SYNTHASE KINASE-3 MODULATORS The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers...

PDB Update 08/21/08

3D4Q
Pyrazole-based inhibitors of B-Raf kinase
Resolution: 2.80 Å

3DB6
Crystal structure of an activated (Thr->Asp) Polo-like kinase 1 (Plk1) catalytic domain in complex with Compound 902
Resolution: 2.85 Å

3DCV
Crystal structure of human Pim1 kinase complexed with 4-(4-hydroxy-3-methyl-phenyl)-6-phenylpyrimidin-2(1H)-one
Resolution: 2.70 Å

Review of Computational Methods - Cephalon

Knowledge Based Prediction of Ligand Binding Modes and Rational Inhibitor Design for Kinase Drug Discovery. Ghose AK, Herbertz T, Pippin DA, Salvino JM, Mallamo JP.

Lck - University of Pittsburgh

Small molecule inhibitors of Lck: the search for specificity within a kinase family. Meyn MA 3rd, Smithgall TE.

Angiokinase - Boehringer Ingelheim

BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ.