Table 1.
Tertiary amine TIQ Rev-erbα agonists
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---|---|---|---|
Compound | R | a Max Inh | EC50 (μM) |
1 | 0.82 | 2.3 | |
3a |
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0.78 | b NT |
3b |
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1.0 | NT |
3c |
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0.90 | NT |
3d |
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1.0 | NT |
3e |
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1.0 | NT |
3f |
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0.95 | NT |
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.