Table 2.
Monoamine oxidase A IC50 values (μM) for the identified β-carbolines.
| Compound | MAO-A Glo | Published a | DYRK1A:MAO-A (IC50 ratio) b |
|---|---|---|---|
| Harmine | 0.06 | 0.003 – 0.107 | 1.2 |
| Harmaline | 0.09 | 0.005 – 0.020 | 26.1 |
| Harmalol | 0.66 | 0.153 | 1.0 |
| Harmol | 0.50 | 0.53 | 0.2 |
| Harmane | 0.64 | 0.029 – 0.337 | 4.2 |
| Tetrahydroharmine | 1.52 | Undetermined | 6.2 |
| Norharmane | 4.29 | 6.47 – 67.1 | 1.3 |
| Staurosporine | No inhibition |
a
(Bálint et al., 2017; Clarke and Ramsay, 2011; Herraiz and Brandt, 2014; Herraiz and Chaparro, 2005; Ionescu et al., 2012; Kim et al., 1997; Rahman and Rahmatullah, 2010; Reniers et al., 2011; Rommelspacher et al., 1994; Rüben et al., 2015; Santillo et al., 2014; Wurzlbauer et al., 2020). Details in Supplementary Table 2.
b
Using TR-FRET DYRK1A IC50 values in this work. As we observed a strong correlation between inhibition potencies in both DYRK1A assay formats, we also see a comparable ranking of DYRK1A:MAO-A ratios if we use the DYRK1A values from the 33P-ATP data.