Table 1 |
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|
In vitro inhibitory activity of CID755673 and its analogs for PKD |
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|
IC50 (nM) |
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|
Compound |
PKD1 |
PKD2 |
PKD3 |
|
|
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|
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) |
|
|
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|
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 |
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LaValle et al. BMC Chemical Biology 2010 10:5 doi:10.1186/1472-6769-10-5 |
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