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. 2021 Jul 15;297(2):100969. doi: 10.1016/j.jbc.2021.100969

Table 1.

Inhibition of P450 17A1 activities: steady-state IC50 values

Inhibitor IC50, nM (95% CI limits)a
Predicted Kib (nM)
Progesterone 17α-hydroxylation 17α-OH pregnenolone lyase Progesterone 17α-hydroxylation 17α-OH pregnenolone lyase
Abiraterone 3.2 (1.7, 6.2) 4.2 (2.6, 6.9) 1.3 3.4
Orteronel 417 (256, 680) 1060 (810, 1400) 160 870
Seviteronel 3500 (2870, 4250) 3430 (2450, 4810) 1370 2810
Ketoconazole 87 (63, 120) 227 (145, 354) 34 190
Clotrimazole 60 (37, 99) 99 (55, 176) 23 81
a

From Figure 3.

b

Using the relationship IC50 = Ki [1 + (S/Km)] for competitive inhibition, with Km values from Ref. (37).