Table 3. Binding of compounds to recombinant T. cruzi CYP51.
Compound | Kd (μM) | I/E2 (5 min) | I/E2 (1 h) |
---|---|---|---|
2 | ND | 4 | 36 |
18 | 0.606 ± 0.023 | 5 | 32 |
19 | 0.023 ± 0.012 | <1 | 3 |
23 | 65.2 ± 5.3 | ND | ND |
Fluconazole | 0.230 ± 0.029 | <1 | 16 |
Bnz* | ND | 43.2 | 45 |
Kd: Dissociation constant. I/E2: Molar ratio of inhibitor/enzyme which causes a 2-fold decrease in enzyme activity in 5 min and 1 hour reactions. ND: Not determined.
Values for Bnz were taken from Ref. [30].