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. Author manuscript; available in PMC: 2020 May 26.
Published in final edited form as: Trends Pharmacol Sci. 2018 Jul 27;39(9):812–827. doi: 10.1016/j.tips.2018.07.003

Table 1.

Circadian clock components and their cognate ligand or small molecule modulators

DRUG NAME CIRCADIAN CLOCK TARGET GENE ACTIVITY References Effect on circadian clock assessed? Y/N
Nobiletin RORs AGONIST [105, 106] Y
SR1001 RORs INVERSE AGONIST [107] Y
SR1078 ROR-α/γ AGONIST [108] N
SR3335 ROR-α INVERSE AGONIST [109] N
SR2211 ROR-γ INVERSE AGONIST [110] N
XY018 ROR-γ INVERSE AGONIST [111] N
XY011/8k ROR-γ ANTAGONIST [112] N
GSK805 ROR-γ ANTAGONIST [113] N
SR 1555 ROR-γ INVERSE AGONIST [114] N
LYC-53772 ROR-γ AGONIST [115] N
LYC-54143 ROR-γ AGONIST [115] N
Ursolic acid ROR-γ INVERSE AGONIST [116] N
Digoxin ROR-γ INVERSE AGONIST [117] N
Compound 1a ROR-γ AGONIST [118] N
Compound 1b ROR-γ AGONIST [118] N
Compound 1c ROR-γ AGONIST [118] N
Inhibitor Y ROR-γ INVERSE AGONIST [118] N
JNJ-54271074 ROR-γ INVERSE AGONIST [119] N
Compound 1 ROR-β and ROR-γ INVERSE AGONIST [120] N
GSK2945 REV-ERBα AGONIST [121] Y
GSK0999 REV-ERBα AGONIST [121] Y
GSK5072 REV-ERBα AGONIST [121] Y
REV-ERBα REV-ERBs ANTAGONIST [122] Y
GSK2667 REV-ERBα AGONIST [121] N
SR9011 REV-ERBs AGONIST [123] Y
SR9009 REV-ERBs AGONIST [123] Y
GSK4112 REV-ERBα AGONIST [124] Y