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. Author manuscript; available in PMC: 2016 Feb 12.
Published in final edited form as: J Med Chem. 2015 Jan 23;58(3):1307–1319. doi: 10.1021/jm5015742

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].