Table 2.
Potent CAMKK2 inhibitors, their IC50 values and calculated selectivity metrics. The method for determination of a given metric was calculated is shown under the method column. The number of kinases used in the calculation is shown in parentheses. The origin of the data is shown under source.
| Inhibitor | IC50 (nM) | Selectivity Metric | Method (#Kinases in Panel) | Source |
|---|---|---|---|---|
| GSK650394 | 3 | 0.083 | S10 @ 1 µM (334) | RBC |
| AP26113 | 16 | 0.125 | IC50 ≤ 50 nM (289) | Literature [101] |
| CDK 1/2 Inhibitor III | 19 | 0.278 | S10 @ 0.5 µM (300) | RBC |
| Lestaurtinib | 25 | 0.356 | Kd ≤ 50 nM (443) | LINCS |
| JAK3 Inhibitor VI | 26 | 0.163 | S10 @ 0.5 µM (300) | RBC |
| ALK-IN-1 | 28 | - | - | |
| STO 609 | 58 | 0.015 | S10 @ 1 µM (409) | KINOMEscan |
| CP 673451 | 73 | - | - | |
| OTSSP167 | 86 | 0.66 | S10 @ 1 µM (141) | MRC |
| BI2536 | 96 | 0.007 | S10 @ 1 µM (131) | MRC |