Table 1 IC50 values of molecules showing antagonistic activity on P2RX7 receptor.

From: A new electro-optical approach for conductance measurement: an assay for the study of drugs acting on ligand-gated ion channels

Compound

ionChannelΩ IC50 (μM)

FLIPR IC50 (μM)

QPatch 16X IC50 (μM)

AXX00179375

8.6

1.59

1.95

AXX00179433

0.31

0.35

0.02

AXX00179853

29.76

27

Inactive

AXX00179861

10.04

1.91

6.51

AXX00179873

3.33

2.2

0.85

AXX00179924

1.77

1.86

1.10

AXX00418759

0.22

0.44

0.02

  1. Within a panel of 30 compounds, designed to act as antagonist on P2RX7 receptor, only 7 showed a measurable activity by one of the following approaches: ionChannelΩ, FLIPR, QPatch 16X. The table reports the IC50 values (double blind measurements) obtained for these 7 compounds on a cell line expressing P2RX7 receptors. IC50 values were calculated by exposing cells to concentrations comprised between 10−4 and 10−9 M and then challenging them with the agonist BzATP (20 μM). n ≥ 3 CRC.
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