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. Author manuscript; available in PMC: 2020 Oct 16.
Published in final edited form as: Bioorg Med Chem. 2010 May 25;18(14):5208–5223. doi: 10.1016/j.bmc.2010.05.057

Table 1.

Effect of the 1-N-substituent on activity profiles

graphic file with name nihms-1634538-t0008.jpg
Compds R IC50 (nM) Ca
assay
T1/2 in rat liver microsomesa
(min)
2 graphic file with name nihms-1634538-t0009.jpg 500 NTb
3 graphic file with name nihms-1634538-t0010.jpg 330 15
4 graphic file with name nihms-1634538-t0011.jpg>3000 12
5 graphic file with name nihms-1634538-t0012.jpg 69 14
6 graphic file with name nihms-1634538-t0013.jpg 54 15
7 graphic file with name nihms-1634538-t0014.jpg 300 NTb
1b graphic file with name nihms-1634538-t0015.jpg 94 12
a

The data show T1/2 after incubating with the 0.2 mg/mL rat liver microsomes.

b

NT: not tested.