Table 2.
Tertiary TIQ amides as Rev-erbα agonists
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---|---|---|---|
Compound | R | a Max Inh | EC50 (μM) |
3g |
![]() |
0.64 | b NT |
3h |
![]() |
0.73 | NT |
3i |
![]() |
0.51 | >3.0 |
3j |
![]() |
0.81 | NT |
3k |
![]() |
0.97 | NT |
3l |
![]() |
0.78 | NT |
3m |
![]() |
0.97 | NT |
3n |
![]() |
1.0 | NT |
3o |
![]() |
0.41 | 2.5 |
3p |
![]() |
0.53 | 2.1 |
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;
NT = not tested.