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Table 1 Potency of 16 in a T47D alkaline phosphatase assays, including Tanaproget (TNP) as a reference compound

From: Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression

compd cLogPc T47D alkaline phosphatase assay EC50 (nM)a T47D alkaline phosphatase assay IC50 (nM)a
TNP 4.16 0.5
1 2.98 > 10,000b 844.8 ± 0.23
2 4.17 4.7 ± 0.07
3 2.98 > 10,000b 795.0 ± 0.25
4 4.17 3674.0 ± 0.08
5 5.02 2294.0 ± 0.29
6 6.18 432.5 ± 0.24
  1. aExperimental values for 1–6 are presented as an average of at least n = 3 measurements ± standard deviation (SD).b The EC50 of 1 and 3 showed no agonist activity so IC50 values were calculated from the inhibition of progesterone (3 mM). c Calculated log P o/w from Chemdraw 12.0