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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 4.

Enzymatic and cellular activities profile of compounds varying R2

Entry R2 mTOR IC50(nM) mTORC1 mTOR IC50(nM) Cellular
8 graphic file with name nihms544302t16.jpg 13.5 40
19 graphic file with name nihms544302t17.jpg 25.8 35
20 graphic file with name nihms544302t18.jpg 239 >300
21 graphic file with name nihms544302t19.jpg 95 200
22 graphic file with name nihms544302t20.jpg 66 250
23 graphic file with name nihms544302t21.jpg 6.84 1
24 graphic file with name nihms544302t22.jpg 3.6 50
25 graphic file with name nihms544302t23.jpg 0.57 5
26 graphic file with name nihms544302t24.jpg 0.29 2
27 graphic file with name nihms544302t25.jpg 389 >300
28 graphic file with name nihms544302t26.jpg 1.26 25
29 graphic file with name nihms544302t27.jpg 21.4 30
30 graphic file with name nihms544302t28.jpg 4.25 5
a

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