Table 2. Dissociation constant Ki and IC50 values of antagonists, isomer B of MLN4760 and DX600, in different samples.
| MLN4760 (Isomer B) | DX600 | |||
|---|---|---|---|---|
|
| ||||
| Enzyme | Ki (μM) | IC50 (μM) | Ki (μM) | IC50 (μM) |
| Recombinant Human ACE2 | 0.04 ± 0.005 | 0.01 ± 0.006 | 0.02 ± 0.008 | 0.01 ± 0.003 |
| Human ACE2 | 0.2 ± 0.01 | 0.5 ± 0.03 | 0.2 ± 0.01 | 0.3 ± 0.05 |
| Murine ACE2 | 2.1 ± 0.2 | 7.1 ± 0.63 | 1.2 ± 0.9 | 0.4 ± 0.07 |
Ki values were determined as described in the text. Assays were repeated four times in case of recombinant ACE2 or carried out in four different samples in case of human and murine cells. IC50 values were obtained from current study as described in the results section.