Table 2. . HSD1169, crenolanib, sorafenib and midostaurin in vitro kinase binding.
| Kinase | HSD1169 ( Kd/nM)† | Crenolanib (Kd/nM)‡ | Sorafenib (Kd/nM)‡ | PKC412 (midostaurin) (Kd/nM)§ |
|---|---|---|---|---|
| FLT3 | 17 | 0.15 | 13 | 11 |
| FLT3-ITD | 0.78 | 0.26 | 95 | 11 |
| FLT3(D835H) | 4.4 | 0.16 | 11 | 6.8 |
| FLT3(D835Y) | 1.1 | 0.14 | 24 | 15 |
| FLT3(D835V) | 1.0 | 3.3 | 140 | – |
| FLT3(ITD, D835V) | 0.41 | 3.6 | 630 | – |
| FLT3(ITD, F691L) | 1.2 | 22 | 860 | – |
| ABL1-phosphorylated | 7200 | 430 | – | – |
| ABL1-nonphosphorylated | 5800 | 140 | 0.33 | – |
†This work: data obtained from KdELECT screening (DiscoverX).
‡Zimmerman et al. [28]. The authors also used KdELECT screening service at DiscoverX.
§Reference Kd provided by DiscoverX.