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. 2010 Oct 22;2(1):2–6. doi: 10.1021/ml100071j

Table 2. Inhibition of CYP11B2 and CYP11B1 by Compounds 2532.

graphic file with name ml-2010-00071j_0006.jpg

    IC50 value (nM)a,b
    IC50 value (nM)a,b
 
n no. CYP11B1 CYP11B2 sfc no. CYP11B1 CYP11B2 sfc
  25 5 30 5.9 26 75 677 9.0
0 27 3 11 3.4 30 >1000 >1000  
1 28 4 8 2.0 31 >1000 >1000  
2 29 80 290 3.6 32 >1000 >1000  
MTPd   15 72 4.8        
ETOd   0.5 0.1 0.2        
KTZd   127 67 0.5        
a

Mean value of at least three experiments. The deviations were within <±25%.

b

Hamster fibroblasts expressing human CYP11B1 or CYP11B2; substrate 11-deoxycorticosterone, 100 nM.

c

sf: IC50 (CYP11B2)/IC50 (CYP11B1).

d

MTP, metyrapone; ETO, etomidate; and KTZ, ketoconazole.