| Assay Method Information | |
| | Biochemical Assay |
| Description: | The activity of the inhibitor compounds against DDR1 and DDR2 was tested using KinaseProfiler (Eurofins). Human DDR1/DDR2 kinase was incubated with 8 mM MOPS buffer (pH=7.0), 0.2 mM EDTA, 250 μM IGF 1Rtide protein kinase substrate (e.g., derived from human IRS-1, and is a substrate for TRK1, JAK2, and RET Kinases enzolifesciences.com/BML-P257/igf-1rtide/), 10 mM Magnesium acetate/Manganese chloride, respectively, and [γ-33P]-ATP. The enzymatic reaction processed in the presence of Mg2+ cations and ATP at room temperature for 40 minutes and terminated by addition of phosphoric acid. The reaction mixture (10 μL) was spotted onto a P30 filtermat and washed four times using 0.425% phosphoric acid and once with methanol. All the compounds were prepared in 100% DMSO. Staurosporine was used as a reference inhibitor and was added to each plate at an estimated concentration resulted in complete inhibition. The results for some of the compounds are listed in Table 1, which shows the ability to inhibit DDR1 and DDR2. As such, these compounds be used as inhibitors of the discoidin domain receptor family, such as for DDR1 and DDR2. However, these compounds may also inhibit other DDR family receptors |
| Affinity data for this assay | |
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