Solution Informationhelp
Enzyme: Focal adhesion kinase 1
inhibitor: BDBM40962
substrate: n/a
 
Solution Type: Aqueous
pH at Preparation: n/a
Temp. Prep.: n/a
Comments: Assay Overview: The purpose of this assay is to determine dose response curves for 210 available out of 212 compounds identified from a previously described set of experiments entitled "Confirmation biochemical assay for inhibitors of Focal Adhesion Kinase (FAK)" (PubChem AID = 794). Each compound was assayed in triplicate using ten 1:3 serial dilutions, starting at a nominal test concentration of 70 micromolar. As with the primary and confirmation screens, a homogeneous time-resolved fluorescence resonance energy transfer (TR-FRET) method to monitor the phosphorylation of a poly Glu-Tyr (poly-GT) substrate by FAK was used to screen for inhibitors. The principle of the assay is similar to other kinase detection systems utilizing TR-FRET, except this method utilizes a FRET acceptor dye which is coupled directly to the substrate. The level of substrate phosphorylation by FAK activity is detected with a specific europium-labeled anti-phospho-peptide antibody (Eu-Ab), which serves as t
 
 

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