Table 1

In vitro inhibitory activity of CID755673 and its analogs for PKD

    IC50 (nM)

Compound

PKD1

PKD2

PKD3


CID755673

182 ± 27 (n = 5)

280 ± 1.8 (n = 3)

227 ± 24 (n = 3)

Kb-NB142-70

28.3 ± 2.3 (n = 3)

58.7 ± 4.2 (n = 3)

53.2 ± 3.5 (n = 3)

Kb-NB165-09

82.5 ± 4.6 (n = 4)

141.6 ± 7.4 (n = 3)

98.5 ± 15.3 (n = 3)

Kb-NB165-31

114.1 ± 23.9 (n = 3)

162.9 ± 20.5 (n = 3)

91.1 ± 17.2 (n = 3)

Kb-NB165-92

111.2 ± 6 (n = 3)

100.7 ± 10.9 (n = 3)

58.8 ± 7.3 (n = 3)

Kb-NB184-02

192.8 ± 27.4 (n = 3)

463.2 ± 38.2 (n = 4)

324.7 ± 39.0 (n = 3)


IC50 were determined for CID755673 and its analogs against PKD1, -2, and -3 using radiometric kinase activity assays. Each IC50 was calculated as the mean ± S.E.M. of at least three independent experiments with triplicate determinations at each concentration in each experiment as described in "Methods." *n, number of independent experiments

LaValle et al. BMC Chemical Biology 2010 10:5   doi:10.1186/1472-6769-10-5

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