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 |