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. 2010 Oct 5;1(9):526–529. doi: 10.1021/ml100198y

Table 1. PHD2 Enzyme Inhibition and Epo Release in Hep3B Cells for Compounds 3a−h.

graphic file with name ml-2010-00198y_0007.jpg

compd R1 R2 R3 R4 pIC50a epo release (%)b
3a H H H H <4 <20
3b Cl Cl H H 4.9 <20
3c Br H H H 4.6 <20
3d F H H H <4 <20
3e OMe H H H 4.3 <20
3f CF3 H CF3 H 4.7 <20
3g CF3 H CF3 (S)-Me 4.3 <20
3h CF3 H CF3 (R)-Me 4.1 <20
a

Negative logarithm of the concentration required to achieve 50% enzyme inhibition; the value is ±0.3 log units.

b

Percent increase in epo release from Hep3B cells at 100 μM concentration relative to positive control measured at 24 h. See the Supporting Information for assay details.