Table 4.

Naphthylamide TIQ Rev-erbα agonists

Compound	R	a Max Inh	EC50 (μM)
3n	⌇–CO2ET	0.41	2.5
4	⌇–CO2H	0.67	b NT
5a	⌇–CONH2	0.61	NT
5b	⌇–CONHPh	0.59	NT
5c	⌇–CONHCH2Ph	0.55	>3.0
6a	⌇–CH2OH	0.71	NT
6b	⌇–CH2OCOCH3	0.65	NT
6c	⌇–CH2OPh	0.37	0.84
6d	⌇–CH2OCH2Ph	0.41	0.65
6e	⌇–CH2O-1-Naphthyl	0.41	1.2
7a	⌇–CH2NH2	0.74	NT
7b	⌇–CH2NHSO2Ph	0.40	NT
7c	⌇–CH2NHCO2CH2Ph	0.53	NT
7d	⌇–CH2NHCH2Ph	0.43	>3.0

^aresults 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;

^bNT = not tested.