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 |
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 |