Table 5.
Comparison of activity (IC) against RpMetAP and HsMetAPs
| Compound | RpMetAP1a,b | HsMetAP1c,d | HsMetAP2c,e |
|---|---|---|---|
| (19) | 1.4 ± 0.1 | >15 | >15 |
| (20) | 1.0 ± 0.3 | >15 | 2.03 ± 0.3 |
| (21) | 0.9 ± 0.1 | 12.9 ± 1.0 | 1.27 ± 0.6 |
| (22) | 1.3 ±0.7 | >15 | 0.055 ± 0.02 |
a
IC50 values in µM
b
IC50 values and standard error obtained from nonlinear regression analysis of the average observed activity (in triplicate) versus inhibitor concentration data.
c
In cases where analysis is limited by compound solubility, the minimum estimate of IC50 is provided, Values from Bhat et al.28
d
Co(II) cofactors employed in assay
e
Mn(II) cofactors employed in assay