Small kinase assay panels can provide a measure of selectivity.
In this Letter, a novel strategy for assessment of ligand promiscuity is described. By using a carefully selected small set of kinases together with multivariate statistical methods, a measure of selectivity can be estimated. This will facilitate an appropriate selection of compounds for further development in lead generation and optimization.
Brandt
Peter
P
Beactica AB, Box 567, SE-751 22 Uppsala, Sweden. Peter.Brandt@beactica.com
Jensen
Annika Jenmalm
AJ
Nilsson
Jonas
J
D015195:Drug Design; D057075:Enzyme Assays; D016018:Least-Squares Analysis; D008024:Ligands; D015999:Multivariate Analysis; D025341:Principal Component Analysis; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D011494:Protein Kinases / Q000737:chemistry* / Q000378:metabolism
D008024:Ligands; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases