TABLE 3.
Current allosteric inhibitors for BCR-ABL and Jak2 that target sites other than the ATP-binding site
| NAME | STRUCTURE | TARGET KINASES | IC50 (nM) | PREDICTED MECHANISM OF INHIBITION | REF. |
|---|---|---|---|---|---|
| GNF-2 |
|
BCR-ABL | 138 | Targets the myristoyl binding cleft | [79] |
| DCC-2036 |
|
BCR-ABL | 5.8 | Targets the switch control pocket | [80] |
| ON012380 |
|
BCR-ABL | 10 | Substrate-competitive | [81] |
| LS104 |
|
Jak2, FLT3 | 1500 (Jak2), 4000 (FLT3) | Substrate-competitive | [87,88] |
| ON044580 |
|
BCR-ABL, Jak2 | 3000 (BCR- ABL), 4000 (Jak2) | Substrate-competitive | [89] |