| Assay Method Information | |
| | In Vitro Assay |
| Description: | Inhibition of LIMK1 and LIMK2. Inhibition of LIMK1 and LIMK2 was measured with Lanthascreen Eu binding assay (Life Technologies). This TR-FRET assay is based on the competition between a fluorescent tracer and the inhibitor to be tested, allowing the determination of an inhibition constant, Ki. 133 compounds have been tested. A dozen of these compounds have their Ki below 10 nM, and about fifty below 50 nM. These results are very promising, as Ki values of the reference compounds LIMKi3 and LX7101 are 8 and 3.9 nM, respectively, and the Pyr1 compound tested on breast cancer tumors has an IC50 of 50 nM on LIMK1 and 75 nM on LIMK2. |
| Affinity data for this assay | |
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