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. Author manuscript; available in PMC: 2013 Jun 1.
Published in final edited form as: Bioorg Med Chem Lett. 2012 Apr 13;22(11):3739–3742. doi: 10.1016/j.bmcl.2012.04.023

Table 2.

Tertiary TIQ amides as Rev-erbα agonists

graphic file with name nihms412702u2.jpg
Compound R a Max Inh EC50 (μM)
3g graphic file with name nihms412702t7.jpg 0.64 b NT
3h graphic file with name nihms412702t8.jpg 0.73 NT
3i graphic file with name nihms412702t9.jpg 0.51 >3.0
3j graphic file with name nihms412702t10.jpg 0.81 NT
3k graphic file with name nihms412702t11.jpg 0.97 NT
3l graphic file with name nihms412702t12.jpg 0.78 NT
3m graphic file with name nihms412702t13.jpg 0.97 NT
3n graphic file with name nihms412702t14.jpg 1.0 NT
3o graphic file with name nihms412702t15.jpg 0.41 2.5
3p graphic file with name nihms412702t16.jpg 0.53 2.1
a

results are average of 2 or more experiments. Value = fold change relative to DMSO control at 10 μM compound. The lower the number, the more efficacious the agonist in terms of repressing transcription;

b

NT = not tested.

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