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. 2012 May 17;3(6):445–449. doi: 10.1021/ml200241a

Table 1. IC50 values for compounds in the CDK enzyme assaysa,b.

graphic file with name ml-2011-00241a_0004.jpg

      IC50 (μM)
  X1 X2 CDK4/Cyclin D1 CDK6/Cyclin D3 CDK1/Cyclin B CDK2/Cyclin A
2 N CH 0.006 ± 0.001 0.049 ± 0.006 1.2 ± 0.2 0.27 ± 0.06
3 N N 0.012 ± 0.002 0.3 ± 0.1 >15 6.2 ± 0.4
4 CCN N 0.003 ± 0.000 0.026 ± 0.003 5.6 ± 0.4 2.4 ± 0.2
5 N CH 0.25 ± 0.03 NT >15 >15
6 CCN N 0.015 ± 0.001 0.12 >15 >15
a

Results are expressed as the mean ± standard deviation of 1–2 IC50 determinations. For each determination, concentration–inhibition curves were obtained in duplicate and then averaged to afford a single IC50 curve with a ≥95% confidence interval.

b

70% homology shared between CDK4 and -6 contributes to comparable SAR profiles of two enzymes.