GSK4112 is an agonist of Rev-erbα with EC50 of 0.4 μM and it can be designed to mimic the action of heme.

SR8278 is a rev-erbα antagonist. It inhibits Rev-Erbα transcriptional repression (EC50 = 0.47 μM) and blocks activity of Rev-Erbα agonist GSK 4112 in HEK293 cells. SR8278 increases expression of glucose-regulating genes, G6Pase and PEPCK in HepG2 cells.

SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively.