| Assay Method Information | |
| | FP Assay |
| Description: | The inhibitory constants (Ki) of the synthesized inhibitors were first determined using a fluorescence polarization (FP)-based competition assay with the previously developed probe II138 as previously reported (Iyamu et al., Anal. Biochem. 2020, 604). Surprisingly, the replacement of the aspartic acid with an acetyl group resulted in a potent bisubstrate inhibitor II399, which displayed a comparable Ki value of 77 nM as our lead compound LL320 (FIG. 2A), whereas II542 containing ethylamine resulted in about a 20-fold reduction in inhibition. |
| Affinity data for this assay | |
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