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. 2011 Apr 17;2(7):515–518. doi: 10.1021/ml200019y

Table 2.

graphic file with name ml-2011-00019y_0004.jpg

    CRTH2 IC50a
compd R in buffer (μM) in plasma (μM)
5 H 0.005 0.060
6 4-F 0.003 0.009
7 3,4-F 0.006 0.015
8 4-Cl 0.007 0.022
9 3-Cl 0.008 0.078
10 2,4-Cl 0.029 0.24
11 4-Me 0.015 0.104
12 4-CF3 0.030 ND
13 4-OCF3 0.070 ND
a

Displacement of 3H-PGD2 from the CRTH2 receptors expressed on HEK 293 cells. Assay run in buffer containing 0.5% bovine serum albumin or in 50% plasma. See ref (26) for assay protocol. Values are the means of three experiments, and the standard deviation is ±30%.