Table 3.
CK1-specific small molecule inhibitors.
| Inhibitor | Structure | IC50 (μM) | ATP (μM) | Reference |
|---|---|---|---|---|
| CKI-7 |  |
CK1: 6 | 100 | (356, 357) |
| IC261 |  |
CK1δ/ε: 2.5 | 100 | (357, 358) |
| D4476 |  |
CK1δ: 0.3 | 100 | (357) |
| Peifer-17 |  |
CK1δ: 0.005; CK1ε: 0.073 | 100 | (31) |
| Peifer-18 |  |
CK1δ: 0.011; CK1ε: 0.447 | 100 | (31) |
| PF-670462 |  |
CK1δ: 0.013; CK1ε: 0.080 | 10 | (273, 359) |
| PF-4800567 |  |
CK1δ: 0.711; CK1ε: 0.032 | 10 | (273) |
| (R)-DRF053 |  |
CK1δ/ε: 0.014 | 15 | (360) |
| 4,5,6,7-Tetrabromo-2-mercaptobenzimidazole |  |
CK1: 2.2 | 20 | (361) |
| 1,4-Diaminoanthra-quinone |  |
CK1δ: 0.3 | Not reported | (362) |
| 1-Hydroxy-4-aminoanthra-quinone |  |
CK1δ: 0.6 | Not reported | (362) |
| (−)-Matairenisol |  |
CK1: 10 | 10 | (363) |
| Lamellarin 3 |  |
CK1δ/ε: 0.41 | 15 | (364) |
| Lamellarin 6 |  |
CK1δ/ε: 0.8 | 15 | (364) |
| SB-202190 |  |
CK1δ: 0.6 | 50 | (365) |
| SR-3029 |  |
CK1δ: 0.044 | 10 | (366) |
| SR-2890 |  |
CK1δ: 0.004 | 10 | (366) |
| Bischof-5 |  |
CK1δ: 0.04; CK1ε: 0.199 | 10 | (367) |
| Bischof-6 |  |
CK1δ: 0.042; CK1ε: 0.033 | 10 | (367) |
| Hua-1h |  |
CK1γ: 0.018 | Not reported | (368) |
| Yang-2 |  |
CK1: 0.078 | Not reported | (369) |
| CK01 | similar to PF-670462 | Not reported | Not reported | (370) |
| MRT00033659 |  |
CK1δ: 0.8935 | 20 | (371) |
| TG0003 |  |
CK1δ: 0.4; CK1ε: 0.55 | Not reported | (277, 372) |
| Salado-34 |  |
CK1δ: 0.01 | 10 | (373) |