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. Author manuscript; available in PMC: 2014 Jan 16.
Published in final edited form as: J Med Chem. 2010 Oct 14;53(19):7146–7155. doi: 10.1021/jm101144f

Table 3.

Enzymatic and cellular activities profile of compounds varying R1

Entry R1 mTOR IC50(nM) mTORC1 mTOR IC50(nM) Cellular
8 graphic file with name nihms544302t5.jpg 13.5 40
9 graphic file with name nihms544302t6.jpg 78.9 100
10 graphic file with name nihms544302t7.jpg 93.8 >300
11 graphic file with name nihms544302t8.jpg 3440 >300
12 graphic file with name nihms544302t9.jpg 33.2 >300
13 graphic file with name nihms544302t10.jpg 662 >300
14 graphic file with name nihms544302t11.jpg 213 >300
15 graphic file with name nihms544302t12.jpg 66.5 150
16 graphic file with name nihms544302t13.jpg 82.6 40
17 graphic file with name nihms544302t14.jpg 45.9 >300
18 graphic file with name nihms544302t15.jpg 214 >300
a

IC50 determinations are the mean of two of independent measurement with standard error of <20%, None of the tested compounds exhibited IC50 for inhibition of cellular PI3K activity of less than 300 nM.

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